Abstract
Depending on the stage of their intervention with the viral replicative cycle, human immunodeficiency virus inhibitors could be divided into the following groups: (i) adsorption inhibitors (i.e., CD4 constructs, polysulfates, polysulfonates, polycarboxylates, and polyoxometalates), (ii) fusion inhibitors (i.e., plant lectins, succinylated or aconitylated albumins, and betulinic acid derivatives), (iii) uncoating inhibitors (i.e., bicyclams), (iv) reverse transcription inhibitors acting either competitively with the substrate binding site (i.e., dideoxynucleoside analogs and acyclic nucleoside phosphonates) or allosterically with a nonsubstrate binding site (i.e., non-nucleoside reverse transcriptase inhibitors), (v) integration inhibitors, (vi) DNA replication inhibitors, (vii) transcription inhibitors (i.e., antisense oligodeoxynucleotides and Tat antagonists), (viii) translation inhibitors (i.e., antisense oligodeoxynucleotides and ribozymes), (ix) maturation inhibitors (i.e., protease inhibitors, myristoylation inhibitors, and glycosylation inhibitors), and finally, (x) budding (assembly/release) inhibitors. Current knowledge, including the therapeutic potential, of these various inhibitors is discussed. In view of their potential clinical the utility, the problem of virus-drug resistance and possible strategies to circumvent this problem are also addressed.
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- Abrams D. I., Goldman A. I., Launer C., Korvick J. A., Neaton J. D., Crane L. R., Grodesky M., Wakefield S., Muth K., Kornegay S. A comparative trial of didanosine or zalcitabine after treatment with zidovudine in patients with human immunodeficiency virus infection. The Terry Beirn Community Programs for Clinical Research on AIDS. N Engl J Med. 1994 Mar 10;330(10):657–662. doi: 10.1056/NEJM199403103301001. [DOI] [PubMed] [Google Scholar]
- Abrams D. I., Kuno S., Wong R., Jeffords K., Nash M., Molaghan J. B., Gorter R., Ueno R. Oral dextran sulfate (UA001) in the treatment of the acquired immunodeficiency syndrome (AIDS) and AIDS-related complex. Ann Intern Med. 1989 Feb 1;110(3):183–188. doi: 10.7326/0003-4819-110-3-183. [DOI] [PubMed] [Google Scholar]
- Agrawal S., Tang J. Y. GEM 91--an antisense oligonucleotide phosphorothioate as a therapeutic agent for AIDS. Antisense Res Dev. 1992 Winter;2(4):261–266. doi: 10.1089/ard.1992.2.261. [DOI] [PubMed] [Google Scholar]
- Alam M., Bechtold C. M., Patick A. K., Skoog M. T., Gant T. G., Colonno R. J., Meyers A. I., Li H., Trimble J., Lin P. F. Substituted naphthalenones as a new structural class of HIV-1 reverse transcriptase inhibitors. Antiviral Res. 1993 Oct;22(2-3):131–141. doi: 10.1016/0166-3542(93)90091-v. [DOI] [PubMed] [Google Scholar]
- Albert J., Wahlberg J., Lundeberg J., Cox S., Sandström E., Wahren B., Uhlén M. Persistence of azidothymidine-resistant human immunodeficiency virus type 1 RNA genotypes in posttreatment sera. J Virol. 1992 Sep;66(9):5627–5630. doi: 10.1128/jvi.66.9.5627-5630.1992. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Althaus I. W., Chou J. J., Gonzales A. J., Deibel M. R., Chou K. C., Kezdy F. J., Romero D. L., Aristoff P. A., Tarpley W. G., Reusser F. Steady-state kinetic studies with the non-nucleoside HIV-1 reverse transcriptase inhibitor U-87201E. J Biol Chem. 1993 Mar 25;268(9):6119–6124. [PubMed] [Google Scholar]
- Andersen D. O., Weber N. D., Wood S. G., Hughes B. G., Murray B. K., North J. A. In vitro virucidal activity of selected anthraquinones and anthraquinone derivatives. Antiviral Res. 1991 Sep;16(2):185–196. doi: 10.1016/0166-3542(91)90024-l. [DOI] [PubMed] [Google Scholar]
- Andrei G., De Clercq E. Molecular approaches for the treatment of hemorrhagic fever virus infections. Antiviral Res. 1993 Sep;22(1):45–75. doi: 10.1016/0166-3542(93)90085-w. [DOI] [PubMed] [Google Scholar]
- Ankel H., Turriziani O., Antonelli G. Prostaglandin A inhibits replication of human immunodeficiency virus during acute infection. J Gen Virol. 1991 Nov;72(Pt 11):2797–2800. doi: 10.1099/0022-1317-72-11-2797. [DOI] [PubMed] [Google Scholar]
- Arnold E., Jacobo-Molina A., Nanni R. G., Williams R. L., Lu X., Ding J., Clark A. D., Jr, Zhang A., Ferris A. L., Clark P. Structure of HIV-1 reverse transcriptase/DNA complex at 7 A resolution showing active site locations. Nature. 1992 May 7;357(6373):85–89. doi: 10.1038/357085a0. [DOI] [PubMed] [Google Scholar]
- Ashkenazi A., Smith D. H., Marsters S. A., Riddle L., Gregory T. J., Ho D. D., Capon D. J. Resistance of primary isolates of human immunodeficiency virus type 1 to soluble CD4 is independent of CD4-rgp120 binding affinity. Proc Natl Acad Sci U S A. 1991 Aug 15;88(16):7056–7060. doi: 10.1073/pnas.88.16.7056. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Ashorn P., Englund G., Martin M. A., Moss B., Berger E. A. Anti-HIV activity of CD4-Pseudomonas exotoxin on infected primary human lymphocytes and monocyte/macrophages. J Infect Dis. 1991 Apr;163(4):703–709. doi: 10.1093/infdis/163.4.703. [DOI] [PubMed] [Google Scholar]
- Ashorn P., Moss B., Weinstein J. N., Chaudhary V. K., FitzGerald D. J., Pastan I., Berger E. A. Elimination of infectious human immunodeficiency virus from human T-cell cultures by synergistic action of CD4-Pseudomonas exotoxin and reverse transcriptase inhibitors. Proc Natl Acad Sci U S A. 1990 Nov;87(22):8889–8893. doi: 10.1073/pnas.87.22.8889. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Aullo P., Alcami J., Popoff M. R., Klatzmann D. R., Murphy J. R., Boquet P. A recombinant diphtheria toxin related human CD4 fusion protein specifically kills HIV infected cells which express gp120 but selects fusion toxin resistant cells which carry HIV. EMBO J. 1992 Feb;11(2):575–583. doi: 10.1002/j.1460-2075.1992.tb05089.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Baba M., De Clercq E., Schols D., Pauwels R., Snoeck R., Van Boeckel C., Van Dedem G., Kraaijeveld N., Hobbelen P., Ottenheijm H. Novel sulfated polysaccharides: dissociation of anti-human immunodeficiency virus activity from antithrombin activity. J Infect Dis. 1990 Feb;161(2):208–213. doi: 10.1093/infdis/161.2.208. [DOI] [PubMed] [Google Scholar]
- Baba M., De Clercq E., Tanaka H., Ubasawa M., Takashima H., Sekiya K., Nitta I., Umezu K., Nakashima H., Mori S. Potent and selective inhibition of human immunodeficiency virus type 1 (HIV-1) by 5-ethyl-6-phenylthiouracil derivatives through their interaction with the HIV-1 reverse transcriptase. Proc Natl Acad Sci U S A. 1991 Mar 15;88(6):2356–2360. doi: 10.1073/pnas.88.6.2356. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Baba M., De Clercq E., Tanaka H., Ubasawa M., Takashima H., Sekiya K., Nitta I., Umezu K., Walker R. T., Mori S. Highly potent and selective inhibition of human immunodeficiency virus type 1 by a novel series of 6-substituted acyclouridine derivatives. Mol Pharmacol. 1991 Jun;39(6):805–810. [PubMed] [Google Scholar]
- Baba M., Ito M., Shigeta S., Tanaka H., Miyasaka T., Ubasawa M., Umezu K., Walker R. T., De Clercq E. Synergistic inhibition of human immunodeficiency virus type 1 replication by 5-ethyl-1-ethoxymethyl-6-(phenylthio)uracil (E-EPU) and azidothymidine in vitro. Antimicrob Agents Chemother. 1991 Jul;35(7):1430–1433. doi: 10.1128/aac.35.7.1430. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Baba M., Kira T., Shigeta S., Matsumoto T., Sawada H. Selective inhibition of human immunodeficiency virus type 1 replication by novel fluoroalkylated oligomers in vitro. J Acquir Immune Defic Syndr. 1994 Jan;7(1):24–30. [PubMed] [Google Scholar]
- Baba M., Konno K., Shigeta S., Wickramasinghe A., Mohan P. Selective inhibition of human cytomegalovirus replication by naphthalenedisulfonic acid derivatives. Antiviral Res. 1993 Mar;20(3):223–233. doi: 10.1016/0166-3542(93)90022-b. [DOI] [PubMed] [Google Scholar]
- Baba M., Pauwels R., Balzarini J., Herdewijn P., De Clercq E., Desmyter J. Ribavirin antagonizes inhibitory effects of pyrimidine 2',3'-dideoxynucleosides but enhances inhibitory effects of purine 2',3'-dideoxynucleosides on replication of human immunodeficiency virus in vitro. Antimicrob Agents Chemother. 1987 Oct;31(10):1613–1617. doi: 10.1128/aac.31.10.1613. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Baba M., Pauwels R., Herdewijn P., De Clercq E., Desmyter J., Vandeputte M. Both 2',3'-dideoxythymidine and its 2',3'-unsaturated derivative (2',3'-dideoxythymidinene) are potent and selective inhibitors of human immunodeficiency virus replication in vitro. Biochem Biophys Res Commun. 1987 Jan 15;142(1):128–134. doi: 10.1016/0006-291x(87)90460-8. [DOI] [PubMed] [Google Scholar]
- Baba M., Schols D., De Clercq E., Pauwels R., Nagy M., Györgyi-Edelényi J., Löw M., Görög S. Novel sulfated polymers as highly potent and selective inhibitors of human immunodeficiency virus replication and giant cell formation. Antimicrob Agents Chemother. 1990 Jan;34(1):134–138. doi: 10.1128/aac.34.1.134. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Baba M., Schols D., Pauwels R., Nakashima H., De Clercq E. Sulfated polysaccharides as potent inhibitors of HIV-induced syncytium formation: a new strategy towards AIDS chemotherapy. J Acquir Immune Defic Syndr. 1990;3(5):493–499. [PubMed] [Google Scholar]
- Baba M., Shigeta S., Yuasa S., Takashima H., Sekiya K., Ubasawa M., Tanaka H., Miyasaka T., Walker R. T., De Clercq E. Preclinical evaluation of MKC-442, a highly potent and specific inhibitor of human immunodeficiency virus type 1 in vitro. Antimicrob Agents Chemother. 1994 Apr;38(4):688–692. doi: 10.1128/aac.38.4.688. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Baba M., Tanaka H., De Clercq E., Pauwels R., Balzarini J., Schols D., Nakashima H., Perno C. F., Walker R. T., Miyasaka T. Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative. Biochem Biophys Res Commun. 1989 Dec 29;165(3):1375–1381. doi: 10.1016/0006-291x(89)92756-3. [DOI] [PubMed] [Google Scholar]
- Baba M., Yuasa S., Niwa T., Yamamoto M., Yabuuchi S., Takashima H., Ubasawa M., Tanaka H., Miyasaka T., Walker R. T. Effect of human serum on the in vitro anti-HIV-1 activity of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) derivatives as related to their lipophilicity and serum protein binding. Biochem Pharmacol. 1993 Jun 22;45(12):2507–2512. doi: 10.1016/0006-2952(93)90232-l. [DOI] [PubMed] [Google Scholar]
- Baboonian C., Dalgleish A., Bountiff L., Gross J., Oroszlan S., Rickett G., Smith-Burchnell C., Troke P., Merson J. HIV-1 proteinase is required for synthesis of pro-viral DNA. Biochem Biophys Res Commun. 1991 Aug 30;179(1):17–24. doi: 10.1016/0006-291x(91)91327-9. [DOI] [PubMed] [Google Scholar]
- Bader J. P., McMahon J. B., Schultz R. J., Narayanan V. L., Pierce J. B., Harrison W. A., Weislow O. S., Midelfort C. F., Stinson S. F., Boyd M. R. Oxathiin carboxanilide, a potent inhibitor of human immunodeficiency virus reproduction. Proc Natl Acad Sci U S A. 1991 Aug 1;88(15):6740–6744. doi: 10.1073/pnas.88.15.6740. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Balzarini J., Hao Z., Herdewijn P., Johns D. G., De Clercq E. Intracellular metabolism and mechanism of anti-retrovirus action of 9-(2-phosphonylmethoxyethyl)adenine, a potent anti-human immunodeficiency virus compound. Proc Natl Acad Sci U S A. 1991 Feb 15;88(4):1499–1503. doi: 10.1073/pnas.88.4.1499. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Balzarini J., Herdewijn P., De Clercq E. Differential patterns of intracellular metabolism of 2',3'-didehydro-2',3'-dideoxythymidine and 3'-azido-2',3'-dideoxythymidine, two potent anti-human immunodeficiency virus compounds. J Biol Chem. 1989 Apr 15;264(11):6127–6133. [PubMed] [Google Scholar]
- Balzarini J., Herdewijn P., De Clercq E. Potentiating effect of ribavirin on the anti-retrovirus activity of 3'-azido-2,6-diaminopurine-2',3'-dideoxyriboside in vitro and in vivo. Antiviral Res. 1989 May-Jun;11(4):161–171. doi: 10.1016/0166-3542(89)90001-6. [DOI] [PubMed] [Google Scholar]
- Balzarini J., Holy A., Jindrich J., Dvorakova H., Hao Z., Snoeck R., Herdewijn P., Johns D. G., De Clercq E. 9-[(2RS)-3-fluoro-2-phosphonylmethoxypropyl] derivatives of purines: a class of highly selective antiretroviral agents in vitro and in vivo. Proc Natl Acad Sci U S A. 1991 Jun 1;88(11):4961–4965. doi: 10.1073/pnas.88.11.4961. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Balzarini J., Holy A., Jindrich J., Naesens L., Snoeck R., Schols D., De Clercq E. Differential antiherpesvirus and antiretrovirus effects of the (S) and (R) enantiomers of acyclic nucleoside phosphonates: potent and selective in vitro and in vivo antiretrovirus activities of (R)-9-(2-phosphonomethoxypropyl)-2,6-diaminopurine. Antimicrob Agents Chemother. 1993 Feb;37(2):332–338. doi: 10.1128/aac.37.2.332. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Balzarini J., Karlsson A., De Clercq E. Human immunodeficiency virus type 1 drug-resistance patterns with different 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives. Mol Pharmacol. 1993 Oct;44(4):694–701. [PubMed] [Google Scholar]
- Balzarini J., Karlsson A., Pérez-Pérez M. J., Camarasa M. J., De Clercq E. Knocking-out concentrations of HIV-1-specific inhibitors completely suppress HIV-1 infection and prevent the emergence of drug-resistant virus. Virology. 1993 Oct;196(2):576–585. doi: 10.1006/viro.1993.1513. [DOI] [PubMed] [Google Scholar]
- Balzarini J., Karlsson A., Pérez-Pérez M. J., Camarasa M. J., Tarpley W. G., De Clercq E. Treatment of human immunodeficiency virus type 1 (HIV-1)-infected cells with combinations of HIV-1-specific inhibitors results in a different resistance pattern than does treatment with single-drug therapy. J Virol. 1993 Sep;67(9):5353–5359. doi: 10.1128/jvi.67.9.5353-5359.1993. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Balzarini J., Karlsson A., Pérez-Pérez M. J., Vrang L., Walbers J., Zhang H., Oberg B., Vandamme A. M., Camarasa M. J., De Clercq E. HIV-1-specific reverse transcriptase inhibitors show differential activity against HIV-1 mutant strains containing different amino acid substitutions in the reverse transcriptase. Virology. 1993 Jan;192(1):246–253. doi: 10.1006/viro.1993.1027. [DOI] [PubMed] [Google Scholar]
- Balzarini J., Karlsson A., Vandamme A. M., Pérez-Pérez M. J., Zhang H., Vrang L., Oberg B., Bäckbro K., Unge T., San-Félix A. Human immunodeficiency virus type 1 (HIV-1) strains selected for resistance against the HIV-1-specific [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro- 5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)]-beta-D-pentofurano syl (TSAO) nucleoside analogues retain sensitivity to HIV-1-specific nonnucleoside inhibitors. Proc Natl Acad Sci U S A. 1993 Aug 1;90(15):6952–6956. doi: 10.1073/pnas.90.15.6952. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Balzarini J., Lee C. K., Herdewijn P., De Clercq E. Mechanism of the potentiating effect of ribavirin on the activity of 2',3'-dideoxyinosine against human immunodeficiency virus. J Biol Chem. 1991 Nov 15;266(32):21509–21514. [PubMed] [Google Scholar]
- Balzarini J., Lee C. K., Schols D., De Clercq E. 1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamide (ribavirin) and 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) markedly potentiate the inhibitory effect of 2',3'-dideoxyinosine on human immunodeficiency virus in peripheral blood lymphocytes. Biochem Biophys Res Commun. 1991 Jul 31;178(2):563–569. doi: 10.1016/0006-291x(91)90145-w. [DOI] [PubMed] [Google Scholar]
- Balzarini J., Mitsuya H., De Clercq E., Broder S. Aurintricarboxylic acid and Evans Blue represent two different classes of anionic compounds which selectively inhibit the cytopathogenicity of human T-cell lymphotropic virus type III/lymphadenopathy-associated virus. Biochem Biophys Res Commun. 1986 Apr 14;136(1):64–71. doi: 10.1016/0006-291x(86)90877-6. [DOI] [PubMed] [Google Scholar]
- Balzarini J., Naesens L., De Clercq E. Anti-retrovirus activity of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in vivo increases when it is less frequently administered. Int J Cancer. 1990 Aug 15;46(2):337–340. doi: 10.1002/ijc.2910460233. [DOI] [PubMed] [Google Scholar]
- Balzarini J., Naesens L., Herdewijn P., Rosenberg I., Holy A., Pauwels R., Baba M., Johns D. G., De Clercq E. Marked in vivo antiretrovirus activity of 9-(2-phosphonylmethoxyethyl)adenine, a selective anti-human immunodeficiency virus agent. Proc Natl Acad Sci U S A. 1989 Jan;86(1):332–336. doi: 10.1073/pnas.86.1.332. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Balzarini J., Naesens L., Robins M. J., De Clercq E. Potentiating effect of ribavirin on the in vitro and in vivo antiretrovirus activities of 2',3'-dideoxyinosine and 2',3'-dideoxy-2,6-diaminopurine riboside. J Acquir Immune Defic Syndr. 1990;3(12):1140–1147. [PubMed] [Google Scholar]
- Balzarini J., Naesens L., Slachmuylders J., Niphuis H., Rosenberg I., Holý A., Schellekens H., De Clercq E. 9-(2-Phosphonylmethoxyethyl)adenine (PMEA) effectively inhibits retrovirus replication in vitro and simian immunodeficiency virus infection in rhesus monkeys. AIDS. 1991 Jan;5(1):21–28. doi: 10.1097/00002030-199101000-00003. [DOI] [PubMed] [Google Scholar]
- Balzarini J., Neyts J., Schols D., Hosoya M., Van Damme E., Peumans W., De Clercq E. The mannose-specific plant lectins from Cymbidium hybrid and Epipactis helleborine and the (N-acetylglucosamine)n-specific plant lectin from Urtica dioica are potent and selective inhibitors of human immunodeficiency virus and cytomegalovirus replication in vitro. Antiviral Res. 1992 Jun;18(2):191–207. doi: 10.1016/0166-3542(92)90038-7. [DOI] [PubMed] [Google Scholar]
- Balzarini J., Pauwels R., Herdewijn P., De Clercq E., Cooney D. A., Kang G. J., Dalal M., Johns D. G., Broder S. Potent and selective anti-HTLV-III/LAV activity of 2',3'-dideoxycytidinene, the 2',3'-unsaturated derivative of 2',3'-dideoxycytidine. Biochem Biophys Res Commun. 1986 Oct 30;140(2):735–742. doi: 10.1016/0006-291x(86)90793-x. [DOI] [PubMed] [Google Scholar]
- Balzarini J., Perno C. F., Schols D., De Clercq E. Activity of acyclic nucleoside phosphonate analogues against human immunodeficiency virus in monocyte/macrophages and peripheral blood lymphocytes. Biochem Biophys Res Commun. 1991 Jul 15;178(1):329–335. doi: 10.1016/0006-291x(91)91818-w. [DOI] [PubMed] [Google Scholar]
- Balzarini J., Pérez-Pérez M. J., San-Félix A., Camarasa M. J., Bathurst I. C., Barr P. J., De Clercq E. Kinetics of inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase by the novel HIV-1-specific nucleoside analogue [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5 "- (4"-amino-1",2"-oxathiole-2",2"-dioxide)thymine (TSAO-T). J Biol Chem. 1992 Jun 15;267(17):11831–11838. [PubMed] [Google Scholar]
- Balzarini J., Pérez-Pérez M. J., San-Félix A., Schols D., Perno C. F., Vandamme A. M., Camarasa M. J., De Clercq E. 2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1'',2''- oxathiole-2'',2'-dioxide)pyrimidine (TSAO) nucleoside analogues: highlyselective inhibitors of human immunodeficiency virus type 1 that are targeted at the viral reverse transcriptase. Proc Natl Acad Sci U S A. 1992 May 15;89(10):4392–4396. doi: 10.1073/pnas.89.10.4392. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Balzarini J., Pérez-Pérez M. J., San-Félix A., Velazquez S., Camarasa M. J., De Clercq E. [2',5'-Bis-O-(tert-butyldimethylsilyl)]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide) (TSAO) derivatives of purine and pyrimidinenucleosides as potent and selective inhibitors of human immunodeficiency virus type 1. Antimicrob Agents Chemother. 1992 May;36(5):1073–1080. doi: 10.1128/aac.36.5.1073. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Balzarini J., Schols D., Neyts J., Van Damme E., Peumans W., De Clercq E. Alpha-(1-3)- and alpha-(1-6)-D-mannose-specific plant lectins are markedly inhibitory to human immunodeficiency virus and cytomegalovirus infections in vitro. Antimicrob Agents Chemother. 1991 Mar;35(3):410–416. doi: 10.1128/aac.35.3.410. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Balzarini J., Sobis H., Naesens L., Vandeputte M., De Clercq E. Inhibitory effects of 9-(2-phosphonylmethoxyethyl)adenine and 3'-azido-2',3'-dideoxythymidine on tumor development in mice inoculated intracerebrally with Moloney murine sarcoma virus. Int J Cancer. 1990 Mar 15;45(3):486–489. doi: 10.1002/ijc.2910450319. [DOI] [PubMed] [Google Scholar]
- Balzarini J., Van Aerschot A., Pauwels R., Baba M., Schols D., Herdewijn P., De Clercq E. 5-Halogeno-3'-fluoro-2',3'-dideoxyuridines as inhibitors of human immunodeficiency virus (HIV): potent and selective anti-HIV activity of 3'-fluoro-2',3'-dideoxy-5-chlorouridine. Mol Pharmacol. 1989 May;35(5):571–577. [PubMed] [Google Scholar]
- Balzarini J., Velazquez S., San-Felix A., Karlsson A., Perez-Perez M. J., Camarasa M. J., De Clercq E. Human immunodeficiency virus type 1-specific [2',5'-bis-O-(tert- butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"- oxathiole-2",2"-dioxide)-purine analogues show a resistance spectrum that is different from that of the human immunodeficiency virus type 1-specific non-nucleoside analogues. Mol Pharmacol. 1993 Jan;43(1):109–114. [PubMed] [Google Scholar]
- Bartolucci C., Cellai L., Di Filippo P., Segre A., Brufani M., Filocamo L., Bianco A. D., Guiso M., Brizzi V., Benedetto A. Rifamycins as inhibitors of retroviral reverse transcriptase from M-MuLV, RAV-2, and HIV-1. Farmaco. 1992 Nov;47(11):1367–1383. [PubMed] [Google Scholar]
- Batinić D., Robey F. A. The V3 region of the envelope glycoprotein of human immunodeficiency virus type 1 binds sulfated polysaccharides and CD4-derived synthetic peptides. J Biol Chem. 1992 Apr 5;267(10):6664–6671. [PubMed] [Google Scholar]
- Berger E. A., Clouse K. A., Chaudhary V. K., Chakrabarti S., FitzGerald D. J., Pastan I., Moss B. CD4-Pseudomonas exotoxin hybrid protein blocks the spread of human immunodeficiency virus infection in vitro and is active against cells expressing the envelope glycoproteins from diverse primate immunodeficiency retroviruses. Proc Natl Acad Sci U S A. 1989 Dec;86(23):9539–9543. doi: 10.1073/pnas.86.23.9539. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Boiziau C., Thuong N. T., Toulmé J. J. Mechanisms of the inhibition of reverse transcription by antisense oligonucleotides. Proc Natl Acad Sci U S A. 1992 Jan 15;89(2):768–772. doi: 10.1073/pnas.89.2.768. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Bordier B., Hélène C., Barr P. J., Litvak S., Sarih-Cottin L. In vitro effect of antisense oligonucleotides on human immunodeficiency virus type 1 reverse transcription. Nucleic Acids Res. 1992 Nov 25;20(22):5999–6006. doi: 10.1093/nar/20.22.5999. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Bos O. J., Vansterkenburg E. L., Boon J. P., Fischer M. J., Wilting J., Janssen L. H. Location and characterization of the suramin binding sites of human serum albumin. Biochem Pharmacol. 1990 Oct 1;40(7):1595–1599. doi: 10.1016/0006-2952(90)90460-3. [DOI] [PubMed] [Google Scholar]
- Boucher C. A., O'Sullivan E., Mulder J. W., Ramautarsing C., Kellam P., Darby G., Lange J. M., Goudsmit J., Larder B. A. Ordered appearance of zidovudine resistance mutations during treatment of 18 human immunodeficiency virus-positive subjects. J Infect Dis. 1992 Jan;165(1):105–110. doi: 10.1093/infdis/165.1.105. [DOI] [PubMed] [Google Scholar]
- Boucher C. A., van Leeuwen R., Kellam P., Schipper P., Tijnagel J., Lange J. M., Larder B. A. Effects of discontinuation of zidovudine treatment on zidovudine sensitivity of human immunodeficiency virus type 1 isolates. Antimicrob Agents Chemother. 1993 Jul;37(7):1525–1530. doi: 10.1128/aac.37.7.1525. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Boyer P. L., Currens M. J., McMahon J. B., Boyd M. R., Hughes S. H. Analysis of nonnucleoside drug-resistant variants of human immunodeficiency virus type 1 reverse transcriptase. J Virol. 1993 Apr;67(4):2412–2420. doi: 10.1128/jvi.67.4.2412-2420.1993. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Boyer P. L., Ding J., Arnold E., Hughes S. H. Subunit specificity of mutations that confer resistance to nonnucleoside inhibitors in human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1994 Sep;38(9):1909–1914. doi: 10.1128/aac.38.9.1909. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Broder S., Yarchoan R., Collins J. M., Lane H. C., Markham P. D., Klecker R. W., Redfield R. R., Mitsuya H., Hoth D. F., Gelmann E. Effects of suramin on HTLV-III/LAV infection presenting as Kaposi's sarcoma or AIDS-related complex: clinical pharmacology and suppression of virus replication in vivo. Lancet. 1985 Sep 21;2(8456):627–630. doi: 10.1016/s0140-6736(85)90002-9. [DOI] [PubMed] [Google Scholar]
- Bryant M. L., Ratner L., Duronio R. J., Kishore N. S., Devadas B., Adams S. P., Gordon J. I. Incorporation of 12-methoxydodecanoate into the human immunodeficiency virus 1 gag polyprotein precursor inhibits its proteolytic processing and virus production in a chronically infected human lymphoid cell line. Proc Natl Acad Sci U S A. 1991 Mar 15;88(6):2055–2059. doi: 10.1073/pnas.88.6.2055. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Buckheit R. W., Jr, Fliakas-Boltz V., Decker W. D., Roberson J. L., Pyle C. A., White E. L., Bowdon B. J., McMahon J. B., Boyd M. R., Bader J. P. Biological and biochemical anti-HIV activity of the benzothiadiazine class of nonnucleoside reverse transcriptase inhibitors. Antiviral Res. 1994 Sep;25(1):43–56. doi: 10.1016/0166-3542(94)90092-2. [DOI] [PubMed] [Google Scholar]
- Buckheit R. W., Jr, Hollingshead M. G., Germany-Decker J., White E. L., McMahon J. B., Allen L. B., Ross L. J., Decker W. D., Westbrook L., Shannon W. M. Thiazolobenzimidazole: biological and biochemical anti-retroviral activity of a new nonnucleoside reverse transcriptase inhibitor. Antiviral Res. 1993 Jul;21(3):247–265. doi: 10.1016/0166-3542(93)90031-d. [DOI] [PubMed] [Google Scholar]
- Bushman F. D., Craigie R. Activities of human immunodeficiency virus (HIV) integration protein in vitro: specific cleavage and integration of HIV DNA. Proc Natl Acad Sci U S A. 1991 Feb 15;88(4):1339–1343. doi: 10.1073/pnas.88.4.1339. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Busso M. E., Resnick L. Anti-human immunodeficiency virus effects of dextran sulfate are strain dependent and synergistic or antagonistic when dextran sulfate is given in combination with dideoxynucleosides. Antimicrob Agents Chemother. 1990 Oct;34(10):1991–1995. doi: 10.1128/aac.34.10.1991. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Byrnes V. W., Emini E. A., Schleif W. A., Condra J. H., Schneider C. L., Long W. J., Wolfgang J. A., Graham D. J., Gotlib L., Schlabach A. J. Susceptibilities of human immunodeficiency virus type 1 enzyme and viral variants expressing multiple resistance-engendering amino acid substitutions to reserve transcriptase inhibitors. Antimicrob Agents Chemother. 1994 Jun;38(6):1404–1407. doi: 10.1128/aac.38.6.1404. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Byrnes V. W., Sardana V. V., Schleif W. A., Condra J. H., Waterbury J. A., Wolfgang J. A., Long W. J., Schneider C. L., Schlabach A. J., Wolanski B. S. Comprehensive mutant enzyme and viral variant assessment of human immunodeficiency virus type 1 reverse transcriptase resistance to nonnucleoside inhibitors. Antimicrob Agents Chemother. 1993 Aug;37(8):1576–1579. doi: 10.1128/aac.37.8.1576. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Bârzu T., Level M., Petitou M., Lormeau J. C., Choay J., Schols D., Baba M., Pauwels R., Witvrouw M., De Clercq E. Preparation and anti-HIV activity of O-acylated heparin and dermatan sulfate derivatives with low anticoagulant effect. J Med Chem. 1993 Nov 12;36(23):3546–3555. doi: 10.1021/jm00075a009. [DOI] [PubMed] [Google Scholar]
- Caliò R., Villani N., Balestra E., Sesa F., Holy A., Balzarini J., De Clercq E., Perno C. F., Del Gobbo V. Enhancement of natural killer activity and interferon induction by different acyclic nucleoside phosphonates. Antiviral Res. 1994 Jan;23(1):77–89. doi: 10.1016/0166-3542(94)90034-5. [DOI] [PubMed] [Google Scholar]
- Callahan L. N., Phelan M., Mallinson M., Norcross M. A. Dextran sulfate blocks antibody binding to the principal neutralizing domain of human immunodeficiency virus type 1 without interfering with gp120-CD4 interactions. J Virol. 1991 Mar;65(3):1543–1550. doi: 10.1128/jvi.65.3.1543-1550.1991. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Cammack N., Rouse P., Marr C. L., Reid P. J., Boehme R. E., Coates J. A., Penn C. R., Cameron J. M. Cellular metabolism of (-) enantiomeric 2'-deoxy-3'-thiacytidine. Biochem Pharmacol. 1992 May 28;43(10):2059–2064. doi: 10.1016/0006-2952(92)90162-c. [DOI] [PubMed] [Google Scholar]
- Campbell T. B., Young R. K., Eron J. J., D'Aquila R. T., Tarpley W. G., Kuritzkes D. R. Inhibition of human immunodeficiency virus type 1 replication in vitro by the bisheteroarylpiperazine atevirdine (U-87201E) in combination with zidovudine or didanosine. J Infect Dis. 1993 Aug;168(2):318–326. doi: 10.1093/infdis/168.2.318. [DOI] [PubMed] [Google Scholar]
- Cantor G. H., McElwain T. F., Birkebak T. A., Palmer G. H. Ribozyme cleaves rex/tax mRNA and inhibits bovine leukemia virus expression. Proc Natl Acad Sci U S A. 1993 Dec 1;90(23):10932–10936. doi: 10.1073/pnas.90.23.10932. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Capon D. J., Chamow S. M., Mordenti J., Marsters S. A., Gregory T., Mitsuya H., Byrn R. A., Lucas C., Wurm F. M., Groopman J. E. Designing CD4 immunoadhesins for AIDS therapy. Nature. 1989 Feb 9;337(6207):525–531. doi: 10.1038/337525a0. [DOI] [PubMed] [Google Scholar]
- Cardin A. D., Smith P. L., Hyde L., Blankenship D. T., Bowlin T. L., Schroeder K., Stauderman K. A., Taylor D. L., Tyms A. S. Stilbene disulfonic acids. CD4 antagonists that block human immunodeficiency virus type-1 growth at multiple stages of the virus life cycle. J Biol Chem. 1991 Jul 15;266(20):13355–13363. [PubMed] [Google Scholar]
- Chatterjee S., Johnson P. R., Wong K. K., Jr Dual-target inhibition of HIV-1 in vitro by means of an adeno-associated virus antisense vector. Science. 1992 Nov 27;258(5087):1485–1488. doi: 10.1126/science.1359646. [DOI] [PubMed] [Google Scholar]
- Cheeseman S. H., Hattox S. E., McLaughlin M. M., Koup R. A., Andrews C., Bova C. A., Pav J. W., Roy T., Sullivan J. L., Keirns J. J. Pharmacokinetics of nevirapine: initial single-rising-dose study in humans. Antimicrob Agents Chemother. 1993 Feb;37(2):178–182. doi: 10.1128/aac.37.2.178. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Chimirri A., Grasso S., Monforte A. M., Monforte P., Zappala M. Anti-HIV agents II. Synthesis and in vitro anti-HIV activity of novel 1H,3H-thiazolo[3,4-a]benzimidazoles. Farmaco. 1991 Jul-Aug;46(7-8):925–933. [PubMed] [Google Scholar]
- Chimirri A., Grasso S., Monforte A. M., Monforte P., Zappalà M. Anti-HIV agents. I: Synthesis and in vitro anti-HIV evaluation of novel 1H,3H-thiazolo[3,4-a]benzimidazoles. Farmaco. 1991 Jun;46(6):817–823. [PubMed] [Google Scholar]
- Chong K. T., Pagano P. J., Hinshaw R. R. Bisheteroarylpiperazine reverse transcriptase inhibitor in combination with 3'-azido-3'-deoxythymidine or 2',3'-dideoxycytidine synergistically inhibits human immunodeficiency virus type 1 replication in vitro. Antimicrob Agents Chemother. 1994 Feb;38(2):288–293. doi: 10.1128/aac.38.2.288. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Chong K. T., Ruwart M. J., Hinshaw R. R., Wilkinson K. F., Rush B. D., Yancey M. F., Strohbach J. W., Thaisrivongs S. Peptidomimetic HIV protease inhibitors: phosphate prodrugs with improved biological activities. J Med Chem. 1993 Aug 20;36(17):2575–2577. doi: 10.1021/jm00069a018. [DOI] [PubMed] [Google Scholar]
- Chow Y. K., Hirsch M. S., Kaplan J. C., D'Aquila R. T. HIV-1 error revealed. Nature. 1993 Aug 19;364(6439):679–679. doi: 10.1038/364679a0. [DOI] [PubMed] [Google Scholar]
- Chow Y. K., Hirsch M. S., Merrill D. P., Bechtel L. J., Eron J. J., Kaplan J. C., D'Aquila R. T. Use of evolutionary limitations of HIV-1 multidrug resistance to optimize therapy. Nature. 1993 Feb 18;361(6413):650–654. doi: 10.1038/361650a0. [DOI] [PubMed] [Google Scholar]
- Ciomei M., Pastori W., Mariani M., Sola F., Grandi M., Mongelli N. New sulfonated distamycin A derivatives with bFGF complexing activity. Biochem Pharmacol. 1994 Jan 20;47(2):295–302. doi: 10.1016/0006-2952(94)90020-5. [DOI] [PubMed] [Google Scholar]
- Clanton D. J., Moran R. A., McMahon J. B., Weislow O. S., Buckheit R. W., Jr, Hollingshead M. G., Ciminale V., Felber B. K., Pavlakis G. N., Bader J. P. Sulfonic acid dyes: inhibition of the human immunodeficiency virus and mechanism of action. J Acquir Immune Defic Syndr. 1992;5(8):771–781. [PubMed] [Google Scholar]
- Cloyd M. W., Lynn W. S., Ramsey K., Baron S. Inhibition of human immunodeficiency virus (HIV-1) infection by diphenylhydantoin (dilantin) implicates role of cellular calcium in virus life cycle. Virology. 1989 Dec;173(2):581–590. doi: 10.1016/0042-6822(89)90569-2. [DOI] [PubMed] [Google Scholar]
- Cohen K. A., Hopkins J., Ingraham R. H., Pargellis C., Wu J. C., Palladino D. E., Kinkade P., Warren T. C., Rogers S., Adams J. Characterization of the binding site for nevirapine (BI-RG-587), a nonnucleoside inhibitor of human immunodeficiency virus type-1 reverse transcriptase. J Biol Chem. 1991 Aug 5;266(22):14670–14674. [PubMed] [Google Scholar]
- Condra J. H., Emini E. A., Gotlib L., Graham D. J., Schlabach A. J., Wolfgang J. A., Colonno R. J., Sardana V. V. Identification of the human immunodeficiency virus reverse transcriptase residues that contribute to the activity of diverse nonnucleoside inhibitors. Antimicrob Agents Chemother. 1992 Jul;36(7):1441–1446. doi: 10.1128/aac.36.7.1441. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Connell E. V., Hsu M. C., Richman D. D. Combinative interactions of a human immunodeficiency virus (HIV) Tat antagonist with HIV reverse transcriptase inhibitors and an HIV protease inhibitor. Antimicrob Agents Chemother. 1994 Feb;38(2):348–352. doi: 10.1128/aac.38.2.348. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Constantoulakis P., Campbell M., Felber B. K., Nasioulas G., Afonina E., Pavlakis G. N. Inhibition of Rev-mediated HIV-1 expression by an RNA binding protein encoded by the interferon-inducible 9-27 gene. Science. 1993 Feb 26;259(5099):1314–1318. doi: 10.1126/science.7680491. [DOI] [PubMed] [Google Scholar]
- Cooper D. A., Pehrson P. O., Pedersen C., Moroni M., Oksenhendler E., Rozenbaum W., Clumeck N., Faber V., Stille W., Hirschel B. The efficacy and safety of zidovudine alone or as cotherapy with acyclovir for the treatment of patients with AIDS and AIDS-related complex: a double-blind randomized trial. European-Australian Collaborative Group. AIDS. 1993 Feb;7(2):197–207. doi: 10.1097/00002030-199302000-00007. [DOI] [PubMed] [Google Scholar]
- Cundy K. C., Shaw J. P., Lee W. A. Oral, subcutaneous, and intramuscular bioavailabilities of the antiviral nucleotide analog 9-(2-phosphonylmethoxyethyl) adenine in cynomolgus monkeys. Antimicrob Agents Chemother. 1994 Feb;38(2):365–368. doi: 10.1128/aac.38.2.365. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Cushman M., Golebiewski W. M., McMahon J. B., Buckheit R. W., Jr, Clanton D. J., Weislow O., Haugwitz R. D., Bader J. P., Graham L., Rice W. G. Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. J Med Chem. 1994 Sep 16;37(19):3040–3050. doi: 10.1021/jm00045a008. [DOI] [PubMed] [Google Scholar]
- Cushman M., Wang P. L., Chang S. H., Wild C., De Clercq E., Schols D., Goldman M. E., Bowen J. A. Preparation and anti-HIV activities of aurintricarboxylic acid fractions and analogues: direct correlation of antiviral potency with molecular weight. J Med Chem. 1991 Jan;34(1):329–337. doi: 10.1021/jm00105a052. [DOI] [PubMed] [Google Scholar]
- Daar E. S., Li X. L., Moudgil T., Ho D. D. High concentrations of recombinant soluble CD4 are required to neutralize primary human immunodeficiency virus type 1 isolates. Proc Natl Acad Sci U S A. 1990 Sep;87(17):6574–6578. doi: 10.1073/pnas.87.17.6574. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Daluge S. M., Purifoy D. J., Savina P. M., St Clair M. H., Parry N. R., Dev I. K., Novak P., Ayers K. M., Reardon J. E., Roberts G. B. 5-Chloro-2',3'-dideoxy-3'-fluorouridine (935U83), a selective anti-human immunodeficiency virus agent with an improved metabolic and toxicological profile. Antimicrob Agents Chemother. 1994 Jul;38(7):1590–1603. doi: 10.1128/aac.38.7.1590. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Davey R. T., Jr, Dewar R. L., Reed G. F., Vasudevachari M. B., Polis M. A., Kovacs J. A., Falloon J., Walker R. E., Masur H., Haneiwich S. E. Plasma viremia as a sensitive indicator of the antiretroviral activity of L-697,661. Proc Natl Acad Sci U S A. 1993 Jun 15;90(12):5608–5612. doi: 10.1073/pnas.90.12.5608. [DOI] [PMC free article] [PubMed] [Google Scholar]
- De Clercq E., Balzarini J. In search of specific inhibitors of retrovirus replication. Antiviral Res. 1985;Suppl 1:89–94. doi: 10.1016/s0166-3542(85)80013-9. [DOI] [PubMed] [Google Scholar]
- De Clercq E. Basic approaches to anti-retroviral treatment. J Acquir Immune Defic Syndr. 1991;4(3):207–218. [PubMed] [Google Scholar]
- De Clercq E. Chemotherapeutic approaches to the treatment of the acquired immune deficiency syndrome (AIDS). J Med Chem. 1986 Sep;29(9):1561–1569. doi: 10.1021/jm00159a001. [DOI] [PubMed] [Google Scholar]
- De Clercq E. HIV inhibitors targeted at the reverse transcriptase. AIDS Res Hum Retroviruses. 1992 Feb;8(2):119–134. doi: 10.1089/aid.1992.8.119. [DOI] [PubMed] [Google Scholar]
- De Clercq E. HIV resistance to reverse transcriptase inhibitors. Biochem Pharmacol. 1994 Jan 20;47(2):155–169. doi: 10.1016/0006-2952(94)90001-9. [DOI] [PubMed] [Google Scholar]
- De Clercq E. HIV-1-specific RT inhibitors: highly selective inhibitors of human immunodeficiency virus type 1 that are specifically targeted at the viral reverse transcriptase. Med Res Rev. 1993 May;13(3):229–258. doi: 10.1002/med.2610130303. [DOI] [PubMed] [Google Scholar]
- De Clercq E. New acquisitions in the development of anti-HIV agents. Antiviral Res. 1989 Aug;12(1):1–19. doi: 10.1016/0166-3542(89)90064-8. [DOI] [PubMed] [Google Scholar]
- De Clercq E. Suramin in the treatment of AIDS: mechanism of action. Antiviral Res. 1987 Jan;7(1):1–10. doi: 10.1016/0166-3542(87)90034-9. [DOI] [PubMed] [Google Scholar]
- De Clercq E. Targets and strategies for the antiviral chemotherapy of AIDS. Trends Pharmacol Sci. 1990 May;11(5):198–205. doi: 10.1016/0165-6147(90)90115-o. [DOI] [PubMed] [Google Scholar]
- De Clercq E., Yamamoto N., Pauwels R., Baba M., Schols D., Nakashima H., Balzarini J., Debyser Z., Murrer B. A., Schwartz D. Potent and selective inhibition of human immunodeficiency virus (HIV)-1 and HIV-2 replication by a class of bicyclams interacting with a viral uncoating event. Proc Natl Acad Sci U S A. 1992 Jun 15;89(12):5286–5290. doi: 10.1073/pnas.89.12.5286. [DOI] [PMC free article] [PubMed] [Google Scholar]
- De Clercq E., Yamamoto N., Pauwels R., Balzarini J., Witvrouw M., De Vreese K., Debyser Z., Rosenwirth B., Peichl P., Datema R. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100. Antimicrob Agents Chemother. 1994 Apr;38(4):668–674. doi: 10.1128/aac.38.4.668. [DOI] [PMC free article] [PubMed] [Google Scholar]
- De Wit S., Hermans P., Sommereijns B., O'Doherty E., Westenborghs R., van de Velde V., Cauwenbergh G. F., Clumeck N. Pharmacokinetics of R 82913 in AIDS patients: a phase I dose-finding study of oral administration compared with intravenous infusion. Antimicrob Agents Chemother. 1992 Dec;36(12):2661–2663. doi: 10.1128/aac.36.12.2661. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Debyser Z., De Vreese K., Pauwels R., Yamamoto N., Anné J., De Clercq E., Desmyter J. Differential inhibitory effects of TIBO derivatives on different strains of simian immunodeficiency virus. J Gen Virol. 1992 Jul;73(Pt 7):1799–1804. doi: 10.1099/0022-1317-73-7-1799. [DOI] [PubMed] [Google Scholar]
- Debyser Z., Pauwels R., Andries K., Desmyter J., Engelborghs Y., Janssen P. A., De Clercq E. Allosteric inhibition of human immunodeficiency virus type 1 reverse transcriptase by tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione compounds. Mol Pharmacol. 1992 Jan;41(1):203–208. [PubMed] [Google Scholar]
- Debyser Z., Pauwels R., Andries K., Desmyter J., Kukla M., Janssen P. A., De Clercq E. An antiviral target on reverse transcriptase of human immunodeficiency virus type 1 revealed by tetrahydroimidazo-[4,5,1-jk] [1,4]benzodiazepin-2 (1H)-one and -thione derivatives. Proc Natl Acad Sci U S A. 1991 Feb 15;88(4):1451–1455. doi: 10.1073/pnas.88.4.1451. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Debyser Z., Pauwels R., Baba M., Desmyter J., De Clercq E. Common features in the interaction of tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione and 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives with the human immunodeficiency virus type 1 reverse transcriptase. Mol Pharmacol. 1992 May;41(5):963–968. [PubMed] [Google Scholar]
- Debyser Z., Vandamme A. M., Pauwels R., Baba M., Desmyter J., De Clercq E. Kinetics of inhibition of endogenous human immunodeficiency virus type 1 reverse transcription by 2',3'-dideoxynucleoside 5'-triphosphate, tetrahydroimidazo-[4,5,1-jk][1,4]-benzodiazepin-2(1H)-thion e, and 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives. J Biol Chem. 1992 Jun 15;267(17):11769–11776. [PubMed] [Google Scholar]
- Dedera D., Vander Heyden N., Ratner L. Attenuation of HIV-1 infectivity by an inhibitor of oligosaccharide processing. AIDS Res Hum Retroviruses. 1990 Jun;6(6):785–794. doi: 10.1089/aid.1990.6.785. [DOI] [PubMed] [Google Scholar]
- Devadas B., Lu T., Katoh A., Kishore N. S., Wade A. C., Mehta P. P., Rudnick D. A., Bryant M. L., Adams S. P., Li Q. Substrate specificity of Saccharomyces cerevisiae myristoyl-CoA: protein N-myristoyltransferase. Analysis of fatty acid analogs containing carbonyl groups, nitrogen heteroatoms, and nitrogen heterocycles in an in vitro enzyme assay and subsequent identification of inhibitors of human immunodeficiency virus I replication. J Biol Chem. 1992 Apr 15;267(11):7224–7239. [PubMed] [Google Scholar]
- Diringer H., Ehlers B. Chemoprophylaxis of scrapie in mice. J Gen Virol. 1991 Feb;72(Pt 2):457–460. doi: 10.1099/0022-1317-72-2-457. [DOI] [PubMed] [Google Scholar]
- Doong S. L., Tsai C. H., Schinazi R. F., Liotta D. C., Cheng Y. C. Inhibition of the replication of hepatitis B virus in vitro by 2',3'-dideoxy-3'-thiacytidine and related analogues. Proc Natl Acad Sci U S A. 1991 Oct 1;88(19):8495–8499. doi: 10.1073/pnas.88.19.8495. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Dornsife R. E., St Clair M. H., Huang A. T., Panella T. J., Koszalka G. W., Burns C. L., Averett D. R. Anti-human immunodeficiency virus synergism by zidovudine (3'-azidothymidine) and didanosine (dideoxyinosine) contrasts with their additive inhibition of normal human marrow progenitor cells. Antimicrob Agents Chemother. 1991 Feb;35(2):322–328. doi: 10.1128/aac.35.2.322. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Dropulić B., Lin N. H., Martin M. A., Jeang K. T. Functional characterization of a U5 ribozyme: intracellular suppression of human immunodeficiency virus type 1 expression. J Virol. 1992 Mar;66(3):1432–1441. doi: 10.1128/jvi.66.3.1432-1441.1992. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Dueweke T. J., Kézdy F. J., Waszak G. A., Deibel M. R., Jr, Tarpley W. G. The binding of a novel bisheteroarylpiperazine mediates inhibition of human immunodeficiency virus type 1 reverse transcriptase. J Biol Chem. 1992 Jan 5;267(1):27–30. [PubMed] [Google Scholar]
- Dueweke T. J., Poppe S. M., Romero D. L., Swaney S. M., So A. G., Downey K. M., Althaus I. W., Reusser F., Busso M., Resnick L. U-90152, a potent inhibitor of human immunodeficiency virus type 1 replication. Antimicrob Agents Chemother. 1993 May;37(5):1127–1131. doi: 10.1128/aac.37.5.1127. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Dueweke T. J., Pushkarskaya T., Poppe S. M., Swaney S. M., Zhao J. Q., Chen I. S., Stevenson M., Tarpley W. G. A mutation in reverse transcriptase of bis(heteroaryl)piperazine-resistant human immunodeficiency virus type 1 that confers increased sensitivity to other nonnucleoside inhibitors. Proc Natl Acad Sci U S A. 1993 May 15;90(10):4713–4717. doi: 10.1073/pnas.90.10.4713. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Durán N., Song P. S. Hypericin and its photodynamic action. Photochem Photobiol. 1986 Jun;43(6):677–680. doi: 10.1111/j.1751-1097.1986.tb05646.x. [DOI] [PubMed] [Google Scholar]
- Egberink H., Borst M., Niphuis H., Balzarini J., Neu H., Schellekens H., De Clercq E., Horzinek M., Koolen M. Suppression of feline immunodeficiency virus infection in vivo by 9-(2-phosphonomethoxyethyl)adenine. Proc Natl Acad Sci U S A. 1990 Apr;87(8):3087–3091. doi: 10.1073/pnas.87.8.3087. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Emini E. A., Graham D. J., Gotlib L., Condra J. H., Byrnes V. W., Schleif W. A. HIV and multidrug resistance. Nature. 1993 Aug 19;364(6439):679–679. doi: 10.1038/364679b0. [DOI] [PubMed] [Google Scholar]
- Erice A., Balfour H. H., Jr, Myers D. E., Leske V. L., Sannerud K. J., Kuebelbeck V., Irvin J. D., Uckun F. M. Anti-human immunodeficiency virus type 1 activity of an anti-CD4 immunoconjugate containing pokeweed antiviral protein. Antimicrob Agents Chemother. 1993 Apr;37(4):835–838. doi: 10.1128/aac.37.4.835. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Erice A., Mayers D. L., Strike D. G., Sannerud K. J., McCutchan F. E., Henry K., Balfour H. H., Jr Brief report: primary infection with zidovudine-resistant human immunodeficiency virus type 1. N Engl J Med. 1993 Apr 22;328(16):1163–1165. doi: 10.1056/NEJM199304223281605. [DOI] [PubMed] [Google Scholar]
- Erickson J., Neidhart D. J., VanDrie J., Kempf D. J., Wang X. C., Norbeck D. W., Plattner J. J., Rittenhouse J. W., Turon M., Wideburg N. Design, activity, and 2.8 A crystal structure of a C2 symmetric inhibitor complexed to HIV-1 protease. Science. 1990 Aug 3;249(4968):527–533. doi: 10.1126/science.2200122. [DOI] [PubMed] [Google Scholar]
- Eriksson B. F., Schinazi R. F. Combinations of 3'-azido-3'-deoxythymidine (zidovudine) and phosphonoformate (foscarnet) against human immunodeficiency virus type 1 and cytomegalovirus replication in vitro. Antimicrob Agents Chemother. 1989 May;33(5):663–669. doi: 10.1128/aac.33.5.663. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Faraj A., Agrofoglio L. A., Wakefield J. K., McPherson S., Morrow C. D., Gosselin G., Mathe C., Imbach J. L., Schinazi R. F., Sommadossi J. P. Inhibition of human immunodeficiency virus type 1 reverse transcriptase by the 5'-triphosphate beta enantiomers of cytidine analogs. Antimicrob Agents Chemother. 1994 Oct;38(10):2300–2305. doi: 10.1128/aac.38.10.2300. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Faulds D., Brogden R. N. Didanosine. A review of its antiviral activity, pharmacokinetic properties and therapeutic potential in human immunodeficiency virus infection. Drugs. 1992 Jul;44(1):94–116. doi: 10.2165/00003495-199244010-00008. [DOI] [PubMed] [Google Scholar]
- Fenouillet E., Gluckman J. C. Effect of a glucosidase inhibitor on the bioactivity and immunoreactivity of human immunodeficiency virus type 1 envelope glycoprotein. J Gen Virol. 1991 Aug;72(Pt 8):1919–1926. doi: 10.1099/0022-1317-72-8-1919. [DOI] [PubMed] [Google Scholar]
- Fenster S. D., Wagner R. W., Froehler B. C., Chin D. J. Inhibition of human immunodeficiency virus type-1 env expression by C-5 propyne oligonucleotides specific for Rev-response element stem-loop V. Biochemistry. 1994 Jul 19;33(28):8391–8398. doi: 10.1021/bi00194a002. [DOI] [PubMed] [Google Scholar]
- Ferrari P., Trabaud M. A., Rommain M., Mandine E., Zalisz R., Desgranges C., Smets P. Toxicity and activity of purified trichosanthin. AIDS. 1991 Jul;5(7):865–870. doi: 10.1097/00002030-199107000-00011. [DOI] [PubMed] [Google Scholar]
- Finberg R. W., Diamond D. C., Mitchell D. B., Rosenstein Y., Soman G., Norman T. C., Schreiber S. L., Burakoff S. J. Prevention of HIV-1 infection and preservation of CD4 function by the binding of CPFs to gp120. Science. 1990 Jul 20;249(4966):287–291. doi: 10.1126/science.2115689. [DOI] [PubMed] [Google Scholar]
- Fischl M. A., Resnick L., Coombs R., Kremer A. B., Pottage J. C., Jr, Fass R. J., Fife K. H., Powderly W. G., Collier A. C., Aspinall R. L. The safety and efficacy of combination N-butyl-deoxynojirimycin (SC-48334) and zidovudine in patients with HIV-1 infection and 200-500 CD4 cells/mm3. J Acquir Immune Defic Syndr. 1994 Feb;7(2):139–147. [PubMed] [Google Scholar]
- Fitzgibbon J. E., Farnham A. E., Sperber S. J., Kim H., Dubin D. T. Human immunodeficiency virus type 1 pol gene mutations in an AIDS patient treated with multiple antiretroviral drugs. J Virol. 1993 Dec;67(12):7271–7275. doi: 10.1128/jvi.67.12.7271-7275.1993. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Fitzgibbon J. E., Howell R. M., Haberzettl C. A., Sperber S. J., Gocke D. J., Dubin D. T. Human immunodeficiency virus type 1 pol gene mutations which cause decreased susceptibility to 2',3'-dideoxycytidine. Antimicrob Agents Chemother. 1992 Jan;36(1):153–157. doi: 10.1128/aac.36.1.153. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Flexner C., Barditch-Crovo P. A., Kornhauser D. M., Farzadegan H., Nerhood L. J., Chaisson R. E., Bell K. M., Lorentsen K. J., Hendrix C. W., Petty B. G. Pharmacokinetics, toxicity, and activity of intravenous dextran sulfate in human immunodeficiency virus infection. Antimicrob Agents Chemother. 1991 Dec;35(12):2544–2550. doi: 10.1128/aac.35.12.2544. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Frank K. B., Noll G. J., Connell E. V., Sim I. S. Kinetic interaction of human immunodeficiency virus type 1 reverse transcriptase with the antiviral tetrahydroimidazo[4,5,1-jk]-[1,4]-benzodiazepine-2-(1H)-thione compound, R82150. J Biol Chem. 1991 Aug 5;266(22):14232–14236. [PubMed] [Google Scholar]
- Fukuma M., Seto Y., Yamase T. In vitro antiviral activity of polyoxotungstate (PM-19) and other polyoxometalates against herpes simplex virus. Antiviral Res. 1991 Dec;16(4):327–339. doi: 10.1016/0166-3542(91)90047-u. [DOI] [PubMed] [Google Scholar]
- Furman P. A., Davis M., Liotta D. C., Paff M., Frick L. W., Nelson D. J., Dornsife R. E., Wurster J. A., Wilson L. J., Fyfe J. A. The anti-hepatitis B virus activities, cytotoxicities, and anabolic profiles of the (-) and (+) enantiomers of cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine. Antimicrob Agents Chemother. 1992 Dec;36(12):2686–2692. doi: 10.1128/aac.36.12.2686. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Furman P. A., Fyfe J. A., St Clair M. H., Weinhold K., Rideout J. L., Freeman G. A., Lehrman S. N., Bolognesi D. P., Broder S., Mitsuya H. Phosphorylation of 3'-azido-3'-deoxythymidine and selective interaction of the 5'-triphosphate with human immunodeficiency virus reverse transcriptase. Proc Natl Acad Sci U S A. 1986 Nov;83(21):8333–8337. doi: 10.1073/pnas.83.21.8333. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Gangemi J. D., Cozens R. M., De Clercq E., Balzarini J., Hochkeppel H. K. 9-(2-Phosphonylmethoxyethyl)adenine in the treatment of murine acquired immunodeficiency disease and opportunistic herpes simplex virus infections. Antimicrob Agents Chemother. 1989 Nov;33(11):1864–1868. doi: 10.1128/aac.33.11.1864. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Gao Q., Gu Z., Parniak M. A., Cameron J., Cammack N., Boucher C., Wainberg M. A. The same mutation that encodes low-level human immunodeficiency virus type 1 resistance to 2',3'-dideoxyinosine and 2',3'-dideoxycytidine confers high-level resistance to the (-) enantiomer of 2',3'-dideoxy-3'-thiacytidine. Antimicrob Agents Chemother. 1993 Jun;37(6):1390–1392. doi: 10.1128/aac.37.6.1390. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Gao W. Y., Han F. S., Storm C., Egan W., Cheng Y. C. Phosphorothioate oligonucleotides are inhibitors of human DNA polymerases and RNase H: implications for antisense technology. Mol Pharmacol. 1992 Feb;41(2):223–229. [PubMed] [Google Scholar]
- Gatti G., Kahn J. O., Lifson J., Williams R., Turin L., Volberding P. A., Gambertoglio J. G. Pharmacokinetics of GLQ223 in rats, monkeys, and patients with AIDS or AIDS-related complex. Antimicrob Agents Chemother. 1991 Dec;35(12):2531–2537. doi: 10.1128/aac.35.12.2531. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Getman D. P., DeCrescenzo G. A., Heintz R. M., Reed K. L., Talley J. J., Bryant M. L., Clare M., Houseman K. A., Marr J. J., Mueller R. A. Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere. J Med Chem. 1993 Jan 22;36(2):288–291. doi: 10.1021/jm00054a014. [DOI] [PubMed] [Google Scholar]
- Ghosh A. K., Thompson W. J., Holloway M. K., McKee S. P., Duong T. T., Lee H. Y., Munson P. M., Smith A. M., Wai J. M., Darke P. L. Potent HIV protease inhibitors: the development of tetrahydrofuranylglycines as novel P2-ligands and pyrazine amides as P3-ligands. J Med Chem. 1993 Aug 6;36(16):2300–2310. doi: 10.1021/jm00068a006. [DOI] [PubMed] [Google Scholar]
- Ghosh A. K., Thompson W. J., Lee H. Y., McKee S. P., Munson P. M., Duong T. T., Darke P. L., Zugay J. A., Emini E. A., Schleif W. A. Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors. J Med Chem. 1993 Apr 2;36(7):924–927. doi: 10.1021/jm00059a019. [DOI] [PubMed] [Google Scholar]
- Ghosh A. K., Thompson W. J., McKee S. P., Duong T. T., Lyle T. A., Chen J. C., Darke P. L., Zugay J. A., Emini E. A., Schleif W. A. 3-Tetrahydrofuran and pyran urethanes as high-affinity P2-ligands for HIV-1 protease inhibitors. J Med Chem. 1993 Jan 22;36(2):292–294. doi: 10.1021/jm00054a015. [DOI] [PubMed] [Google Scholar]
- Goldfeld A. E., Flemington E. K., Boussiotis V. A., Theodos C. M., Titus R. G., Strominger J. L., Speck S. H. Transcription of the tumor necrosis factor alpha gene is rapidly induced by anti-immunoglobulin and blocked by cyclosporin A and FK506 in human B cells. Proc Natl Acad Sci U S A. 1992 Dec 15;89(24):12198–12201. doi: 10.1073/pnas.89.24.12198. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Goldman M. E., Nunberg J. H., O'Brien J. A., Quintero J. C., Schleif W. A., Freund K. F., Gaul S. L., Saari W. S., Wai J. S., Hoffman J. M. Pyridinone derivatives: specific human immunodeficiency virus type 1 reverse transcriptase inhibitors with antiviral activity. Proc Natl Acad Sci U S A. 1991 Aug 1;88(15):6863–6867. doi: 10.1073/pnas.88.15.6863. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Goldman M. E., O'Brien J. A., Ruffing T. L., Nunberg J. H., Schleif W. A., Quintero J. C., Siegl P. K., Hoffman J. M., Smith A. M., Emini E. A. L-696,229 specifically inhibits human immunodeficiency virus type 1 reverse transcriptase and possesses antiviral activity in vitro. Antimicrob Agents Chemother. 1992 May;36(5):1019–1023. doi: 10.1128/aac.36.5.1019. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Goldman M. E., O'Brien J. A., Ruffing T. L., Schleif W. A., Sardana V. V., Byrnes V. W., Condra J. H., Hoffman J. M., Emini E. A. A nonnucleoside reverse transcriptase inhibitor active on human immunodeficiency virus type 1 isolates resistant to related inhibitors. Antimicrob Agents Chemother. 1993 May;37(5):947–949. doi: 10.1128/aac.37.5.947. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Goldman M. E., Salituro G. S., Bowen J. A., Williamson J. M., Zink D. L., Schleif W. A., Emini E. A. Inhibition of human immunodeficiency virus-1 reverse transcriptase activity by rubromycins: competitive interaction at the template.primer site. Mol Pharmacol. 1990 Jul;38(1):20–25. [PubMed] [Google Scholar]
- Gosselin G., Schinazi R. F., Sommadossi J. P., Mathé C., Bergogne M. C., Aubertin A. M., Kirn A., Imbach J. L. Anti-human immunodeficiency virus activities of the beta-L enantiomer of 2',3'-dideoxycytidine and its 5-fluoro derivative in vitro. Antimicrob Agents Chemother. 1994 Jun;38(6):1292–1297. doi: 10.1128/aac.38.6.1292. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Gruters R. A., Neefjes J. J., Tersmette M., de Goede R. E., Tulp A., Huisman H. G., Miedema F., Ploegh H. L. Interference with HIV-induced syncytium formation and viral infectivity by inhibitors of trimming glucosidase. Nature. 1987 Nov 5;330(6143):74–77. doi: 10.1038/330074a0. [DOI] [PubMed] [Google Scholar]
- Gu Z., Gao Q., Fang H., Salomon H., Parniak M. A., Goldberg E., Cameron J., Wainberg M. A. Identification of a mutation at codon 65 in the IKKK motif of reverse transcriptase that encodes human immunodeficiency virus resistance to 2',3'-dideoxycytidine and 2',3'-dideoxy-3'-thiacytidine. Antimicrob Agents Chemother. 1994 Feb;38(2):275–281. doi: 10.1128/aac.38.2.275. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Gu Z., Gao Q., Li X., Parniak M. A., Wainberg M. A. Novel mutation in the human immunodeficiency virus type 1 reverse transcriptase gene that encodes cross-resistance to 2',3'-dideoxyinosine and 2',3'-dideoxycytidine. J Virol. 1992 Dec;66(12):7128–7135. doi: 10.1128/jvi.66.12.7128-7135.1992. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Guo L., Heinzinger N. K., Stevenson M., Schopfer L. M., Salhany J. M. Inhibition of gp120-CD4 interaction and human immunodeficiency virus type 1 infection in vitro by pyridoxal 5'-phosphate. Antimicrob Agents Chemother. 1994 Oct;38(10):2483–2487. doi: 10.1128/aac.38.10.2483. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Gupta P., Balachandran R., Thampatty P., Rinaldo C., Ho M. Oxophenarsine, an antisyphilis drug inhibits HIV-1-specific protein synthesis in acutely and persistently infected lymphocytes. AIDS Res Hum Retroviruses. 1990 Dec;6(12):1417–1423. doi: 10.1089/aid.1990.6.1417. [DOI] [PubMed] [Google Scholar]
- Göttlinger H. G., Sodroski J. G., Haseltine W. A. Role of capsid precursor processing and myristoylation in morphogenesis and infectivity of human immunodeficiency virus type 1. Proc Natl Acad Sci U S A. 1989 Aug;86(15):5781–5785. doi: 10.1073/pnas.86.15.5781. [DOI] [PMC free article] [PubMed] [Google Scholar]
- HIV seroconversion after occupational exposure despite early prophylactic zidovudine therapy. Lancet. 1993 Apr 24;341(8852):1077–1078. [PubMed] [Google Scholar]
- Hafkemeyer P., Neftel K., Hobi R., Pfaltz A., Lutz H., Lüthi K., Focher F., Spadari S., Hübscher U. HP 0.35, a cephalosporin degradation product is a specific inhibitor of lentiviral RNAses H. Nucleic Acids Res. 1991 Aug 11;19(15):4059–4065. doi: 10.1093/nar/19.15.4059. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hamamoto Y., Nakashima H., Matsui T., Matsuda A., Ueda T., Yamamoto N. Inhibitory effect of 2',3'-didehydro-2',3'-dideoxynucleosides on infectivity, cytopathic effects, and replication of human immunodeficiency virus. Antimicrob Agents Chemother. 1987 Jun;31(6):907–910. doi: 10.1128/aac.31.6.907. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Handa A., Hoshino H., Nakajima K., Adachi M., Ikeda K., Achiwa K., Itoh T., Suzuki Y. Inhibition of infection with human immunodeficiency virus type 1 by sulfated gangliosides. Biochem Biophys Res Commun. 1991 Feb 28;175(1):1–9. doi: 10.1016/s0006-291x(05)81191-x. [DOI] [PubMed] [Google Scholar]
- Hao Z., Cooney D. A., Farquhar D., Perno C. F., Zhang K., Masood R., Wilson Y., Hartman N. R., Balzarini J., Johns D. G. Potent DNA chain termination activity and selective inhibition of human immunodeficiency virus reverse transcriptase by 2',3'-dideoxyuridine-5'-triphosphate. Mol Pharmacol. 1990 Feb;37(2):157–163. [PubMed] [Google Scholar]
- Hao Z., Cooney D. A., Hartman N. R., Perno C. F., Fridland A., DeVico A. L., Sarngadharan M. G., Broder S., Johns D. G. Factors determining the activity of 2',3'-dideoxynucleosides in suppressing human immunodeficiency virus in vitro. Mol Pharmacol. 1988 Oct;34(4):431–435. [PubMed] [Google Scholar]
- Harakeh S., Jariwalla R. J., Pauling L. Suppression of human immunodeficiency virus replication by ascorbate in chronically and acutely infected cells. Proc Natl Acad Sci U S A. 1990 Sep;87(18):7245–7249. doi: 10.1073/pnas.87.18.7245. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Harmenberg J., Akesson-Johansson A., Vrang L., Cox S. Synergistic inhibition of human immunodeficiency virus replication in vitro by combinations of 3'-azido-3'-deoxythymidine and 3'-fluoro-3'-deoxythymidine. AIDS Res Hum Retroviruses. 1990 Oct;6(10):1197–1202. doi: 10.1089/aid.1990.6.1197. [DOI] [PubMed] [Google Scholar]
- Harrington J. A., Reardon J. E., Spector T. 3'-azido-3'-deoxythymidine (AZT) monophosphate: an inhibitor of exonucleolytic repair of AZT-terminated DNA. Antimicrob Agents Chemother. 1993 Apr;37(4):918–920. doi: 10.1128/aac.37.4.918. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Harrison G. S., Long C. J., Maxwell F., Glode L. M., Maxwell I. H. Inhibition of HIV production in cells containing an integrated, HIV-regulated diphtheria toxin A chain gene. AIDS Res Hum Retroviruses. 1992 Jan;8(1):39–45. doi: 10.1089/aid.1992.8.39. [DOI] [PubMed] [Google Scholar]
- Hartman N. R., Ahluwalia G. S., Cooney D. A., Mitsuya H., Kageyama S., Fridland A., Broder S., Johns D. G. Inhibitors of IMP dehydrogenase stimulate the phosphorylation of the anti-human immunodeficiency virus nucleosides 2',3'-dideoxyadenosine and 2',3'-dideoxyinosine. Mol Pharmacol. 1991 Jul;40(1):118–124. [PubMed] [Google Scholar]
- Hartman N. R., Johns D. G., Mitsuya H. Pharmacokinetic analysis of dextran sulfate in rats as pertains to its clinical usefulness for therapy of HIV infection. AIDS Res Hum Retroviruses. 1990 Jun;6(6):805–812. doi: 10.1089/aid.1990.6.805. [DOI] [PubMed] [Google Scholar]
- Hartshorn K. L., Sandstrom E. G., Neumeyer D., Paradis T. J., Chou T. C., Schooley R. T., Hirsch M. S. Synergistic inhibition of human T-cell lymphotropic virus type III replication in vitro by phosphonoformate and recombinant alpha-A interferon. Antimicrob Agents Chemother. 1986 Jul;30(1):189–191. doi: 10.1128/aac.30.1.189. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hartshorn K. L., Vogt M. W., Chou T. C., Blumberg R. S., Byington R., Schooley R. T., Hirsch M. S. Synergistic inhibition of human immunodeficiency virus in vitro by azidothymidine and recombinant alpha A interferon. Antimicrob Agents Chemother. 1987 Feb;31(2):168–172. doi: 10.1128/aac.31.2.168. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hatanaka K., Yoshida T., Uryu T., Yoshida O., Nakashima H., Yamamoto N., Mimura T., Kaneko Y. Synthesis of an inhibitor of human immunodeficiency virus infection. Jpn J Cancer Res. 1989 Feb;80(2):95–98. doi: 10.1111/j.1349-7006.1989.tb02272.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hayashi S., Fine R. L., Chou T. C., Currens M. J., Broder S., Mitsuya H. In vitro inhibition of the infectivity and replication of human immunodeficiency virus type 1 by combination of antiretroviral 2',3'-dideoxynucleosides and virus-binding inhibitors. Antimicrob Agents Chemother. 1990 Jan;34(1):82–88. doi: 10.1128/aac.34.1.82. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Heidenreich O., Benseler F., Fahrenholz A., Eckstein F. High activity and stability of hammerhead ribozymes containing 2'-modified pyrimidine nucleosides and phosphorothioates. J Biol Chem. 1994 Jan 21;269(3):2131–2138. [PubMed] [Google Scholar]
- Heidenreich O., Eckstein F. Hammerhead ribozyme-mediated cleavage of the long terminal repeat RNA of human immunodeficiency virus type 1. J Biol Chem. 1992 Jan 25;267(3):1904–1909. [PubMed] [Google Scholar]
- Heijtink R. A., De Wilde G. A., Kruining J., Berk L., Balzarini J., De Clercq E., Holy A., Schalm S. W. Inhibitory effect of 9-(2-phosphonylmethoxyethyl)-adenine (PMEA) on human and duck hepatitis B virus infection. Antiviral Res. 1993 Jun;21(2):141–153. doi: 10.1016/0166-3542(93)90050-s. [DOI] [PubMed] [Google Scholar]
- Herrmann C. H., Rice A. P. Specific interaction of the human immunodeficiency virus Tat proteins with a cellular protein kinase. Virology. 1993 Dec;197(2):601–608. doi: 10.1006/viro.1993.1634. [DOI] [PubMed] [Google Scholar]
- Hill C. L., Weeks M. S., Schinazi R. F. Anti-HIV-1 activity, toxicity, and stability studies of representative structural families of polyoxometalates. J Med Chem. 1990 Oct;33(10):2767–2772. doi: 10.1021/jm00172a014. [DOI] [PubMed] [Google Scholar]
- Hizi A., Tal R., Shaharabany M., Currens M. J., Boyd M. R., Hughes S. H., McMahon J. B. Specific inhibition of the reverse transcriptase of human immunodeficiency virus type 1 and the chimeric enzymes of human immunodeficiency virus type 1 and type 2 by nonnucleoside inhibitors. Antimicrob Agents Chemother. 1993 May;37(5):1037–1042. doi: 10.1128/aac.37.5.1037. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Ho H. T., Hitchcock M. J. Cellular pharmacology of 2',3'-dideoxy-2',3'-didehydrothymidine, a nucleoside analog active against human immunodeficiency virus. Antimicrob Agents Chemother. 1989 Jun;33(6):844–849. doi: 10.1128/aac.33.6.844. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Holmes D. S., Bethell R. C., Cammack N., Clemens I. R., Kitchin J., McMeekin P., Mo C. L., Orr D. C., Patel B., Paternoster I. L. Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors containing a stereochemically unique peptide isostere. J Med Chem. 1993 Oct 15;36(21):3129–3136. doi: 10.1021/jm00073a012. [DOI] [PubMed] [Google Scholar]
- Hoover E. A., Ebner J. P., Zeidner N. S., Mullins J. I. Early therapy of feline leukemia virus infection (FeLV-FAIDS) with 9-(2-phosphonylmethoxyethyl)adenine (PMEA). Antiviral Res. 1991 Jul;16(1):77–92. doi: 10.1016/0166-3542(91)90060-5. [DOI] [PubMed] [Google Scholar]
- Hosoya M., Balzarini J., Shigeta S., De Clercq E. Differential inhibitory effects of sulfated polysaccharides and polymers on the replication of various myxoviruses and retroviruses, depending on the composition of the target amino acid sequences of the viral envelope glycoproteins. Antimicrob Agents Chemother. 1991 Dec;35(12):2515–2520. doi: 10.1128/aac.35.12.2515. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hsu M. C., Dhingra U., Earley J. V., Holly M., Keith D., Nalin C. M., Richou A. R., Schutt A. D., Tam S. Y., Potash M. J. Inhibition of type 1 human immunodeficiency virus replication by a tat antagonist to which the virus remains sensitive after prolonged exposure in vitro. Proc Natl Acad Sci U S A. 1993 Jul 15;90(14):6395–6399. doi: 10.1073/pnas.90.14.6395. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hsu M. C., Schutt A. D., Holly M., Slice L. W., Sherman M. I., Richman D. D., Potash M. J., Volsky D. J. Inhibition of HIV replication in acute and chronic infections in vitro by a Tat antagonist. Science. 1991 Dec 20;254(5039):1799–1802. doi: 10.1126/science.1763331. [DOI] [PubMed] [Google Scholar]
- Huang P., Farquhar D., Plunkett W. Selective action of 3'-azido-3'-deoxythymidine 5'-triphosphate on viral reverse transcriptases and human DNA polymerases. J Biol Chem. 1990 Jul 15;265(20):11914–11918. [PubMed] [Google Scholar]
- Hudson J. B., Lopez-Bazzocchi I., Towers G. H. Antiviral activities of hypericin. Antiviral Res. 1991 Feb;15(2):101–112. doi: 10.1016/0166-3542(91)90028-p. [DOI] [PubMed] [Google Scholar]
- Humber D. C., Bamford M. J., Bethell R. C., Cammack N., Cobley K., Evans D. N., Gray N. M., Hann M. M., Orr D. C., Saunders J. A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships. J Med Chem. 1993 Oct 15;36(21):3120–3128. doi: 10.1021/jm00073a011. [DOI] [PubMed] [Google Scholar]
- Inouye Y., Tokutake Y., Yoshida T., Seto Y., Hujita H., Dan K., Yamamoto A., Nishiya S., Yamase T., Nakamura S. In vitro antiviral activity of polyoxomolybdates. Mechanism of inhibitory effect of PM-104 (NH4)12H2(Eu4(MoO4)(H2O)16(Mo7O24)4).13H2O on human immunodeficiency virus type 1. Antiviral Res. 1993 Apr;20(4):317–331. doi: 10.1016/0166-3542(93)90075-t. [DOI] [PubMed] [Google Scholar]
- Ito M., Baba M., Shigeta S., De Clercq E., Walker R. T., Tanaka H., Miyasaka T. Synergistic inhibition of human immunodeficiency virus type 1 (HIV-1) replication in vitro by 1-[(2-hydroxyethoxy)methyl]-6-phenylthiothymine (HEPT) and recombinant alpha interferon. Antiviral Res. 1991 May;15(4):323–330. doi: 10.1016/0166-3542(91)90013-h. [DOI] [PubMed] [Google Scholar]
- Jacobo-Molina A., Ding J., Nanni R. G., Clark A. D., Jr, Lu X., Tantillo C., Williams R. L., Kamer G., Ferris A. L., Clark P. Crystal structure of human immunodeficiency virus type 1 reverse transcriptase complexed with double-stranded DNA at 3.0 A resolution shows bent DNA. Proc Natl Acad Sci U S A. 1993 Jul 1;90(13):6320–6324. doi: 10.1073/pnas.90.13.6320. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Jansen R. W., Molema G., Pauwels R., Schols D., De Clercq E., Meijer D. K. Potent in vitro anti-human immunodeficiency virus-1 activity of modified human serum albumins. Mol Pharmacol. 1991 Jun;39(6):818–823. [PubMed] [Google Scholar]
- Jansen R. W., Schols D., Pauwels R., De Clercq E., Meijer D. K. Novel, negatively charged, human serum albumins display potent and selective in vitro anti-human immunodeficiency virus type 1 activity. Mol Pharmacol. 1993 Nov;44(5):1003–1007. [PubMed] [Google Scholar]
- Jentsch K. D., Hunsmann G., Hartmann H., Nickel P. Inhibition of human immunodeficiency virus type I reverse transcriptase by suramin-related compounds. J Gen Virol. 1987 Aug;68(Pt 8):2183–2192. doi: 10.1099/0022-1317-68-8-2183. [DOI] [PubMed] [Google Scholar]
- Johns D. G., Ahluwalia G. S., Cooney D. A., Mitsuya H., Driscoll J. S. Enhanced stimulation by ribavirin of the 5'-phosphorylation and anti-human immunodeficiency virus activity of purine 2'-beta-fluoro-2',3'-dideoxynucleosides. Mol Pharmacol. 1993 Sep;44(3):519–523. [PubMed] [Google Scholar]
- Johnson V. A., Barlow M. A., Chou T. C., Fisher R. A., Walker B. D., Hirsch M. S., Schooley R. T. Synergistic inhibition of human immunodeficiency virus type 1 (HIV-1) replication in vitro by recombinant soluble CD4 and 3'-azido-3'-deoxythymidine. J Infect Dis. 1989 May;159(5):837–844. doi: 10.1093/infdis/159.5.837. [DOI] [PubMed] [Google Scholar]
- Johnson V. A., Barlow M. A., Merrill D. P., Chou T. C., Hirsch M. S. Three-drug synergistic inhibition of HIV-1 replication in vitro by zidovudine, recombinant soluble CD4, and recombinant interferon-alpha A. J Infect Dis. 1990 Jun;161(6):1059–1067. doi: 10.1093/infdis/161.6.1059. [DOI] [PubMed] [Google Scholar]
- Johnson V. A., Merrill D. P., Videler J. A., Chou T. C., Byington R. E., Eron J. J., D'Aquila R. T., Hirsch M. S. Two-drug combinations of zidovudine, didanosine, and recombinant interferon-alpha A inhibit replication of zidovudine-resistant human immunodeficiency virus type 1 synergistically in vitro. J Infect Dis. 1991 Oct;164(4):646–655. doi: 10.1093/infdis/164.4.646. [DOI] [PubMed] [Google Scholar]
- Johnson V. A., Walker B. D., Barlow M. A., Paradis T. J., Chou T. C., Hirsch M. S. Synergistic inhibition of human immunodeficiency virus type 1 and type 2 replication in vitro by castanospermine and 3'-azido-3'-deoxythymidine. Antimicrob Agents Chemother. 1989 Jan;33(1):53–57. doi: 10.1128/aac.33.1.53. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Johnston M. I., Hoth D. F. Present status and future prospects for HIV therapies. Science. 1993 May 28;260(5112):1286–1293. doi: 10.1126/science.7684163. [DOI] [PubMed] [Google Scholar]
- Jonckheere H., Taymans J. M., Balzarini J., Velázquez S., Camarasa M. J., Desmyter J., De Clercq E., Anné J. Resistance of HIV-1 reverse transcriptase against [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1'',2''- oxathiole-2'',2''-dioxide)] (TSAO) derivatives is determined by the mutation Glu138-->Lys on the p51 subunit. J Biol Chem. 1994 Oct 14;269(41):25255–25258. [PubMed] [Google Scholar]
- Kageyama S., Mimoto T., Murakawa Y., Nomizu M., Ford H., Jr, Shirasaka T., Gulnik S., Erickson J., Takada K., Hayashi H. In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine. Antimicrob Agents Chemother. 1993 Apr;37(4):810–817. doi: 10.1128/aac.37.4.810. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kageyama S., Weinstein J. N., Shirasaka T., Kempf D. J., Norbeck D. W., Plattner J. J., Erickson J., Mitsuya H. In vitro inhibition of human immunodeficiency virus (HIV) type 1 replication by C2 symmetry-based HIV protease inhibitors as single agents or in combinations. Antimicrob Agents Chemother. 1992 May;36(5):926–933. doi: 10.1128/aac.36.5.926. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kahn J. O., Lagakos S. W., Richman D. D., Cross A., Pettinelli C., Liou S. H., Brown M., Volberding P. A., Crumpacker C. S., Beall G. A controlled trial comparing continued zidovudine with didanosine in human immunodeficiency virus infection. The NIAID AIDS Clinical Trials Group. N Engl J Med. 1992 Aug 27;327(9):581–587. doi: 10.1056/NEJM199208273270901. [DOI] [PubMed] [Google Scholar]
- Kalebic T., Kinter A., Poli G., Anderson M. E., Meister A., Fauci A. S. Suppression of human immunodeficiency virus expression in chronically infected monocytic cells by glutathione, glutathione ester, and N-acetylcysteine. Proc Natl Acad Sci U S A. 1991 Feb 1;88(3):986–990. doi: 10.1073/pnas.88.3.986. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Karn J., Graeble M. A. New insights into the mechanism of HIV-1 trans-activation. Trends Genet. 1992 Nov;8(11):365–368. doi: 10.1016/0168-9525(92)90284-b. [DOI] [PubMed] [Google Scholar]
- Karpas A., Fleet G. W., Dwek R. A., Petursson S., Namgoong S. K., Ramsden N. G., Jacob G. S., Rademacher T. W. Aminosugar derivatives as potential anti-human immunodeficiency virus agents. Proc Natl Acad Sci U S A. 1988 Dec;85(23):9229–9233. doi: 10.1073/pnas.85.23.9229. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Karpas A., Lowdell M., Jacobson S. K., Hill F. Inhibition of human immunodeficiency virus and growth of infected T cells by the immunosuppressive drugs cyclosporin A and FK 506. Proc Natl Acad Sci U S A. 1992 Sep 1;89(17):8351–8355. doi: 10.1073/pnas.89.17.8351. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kashman Y., Gustafson K. R., Fuller R. W., Cardellina J. H., 2nd, McMahon J. B., Currens M. J., Buckheit R. W., Jr, Hughes S. H., Cragg G. M., Boyd M. R. The calanolides, a novel HIV-inhibitory class of coumarin derivatives from the tropical rainforest tree, Calophyllum lanigerum. J Med Chem. 1992 Jul 24;35(15):2735–2743. doi: 10.1021/jm00093a004. [DOI] [PubMed] [Google Scholar]
- Kawasaki A. M., Casper M. D., Freier S. M., Lesnik E. A., Zounes M. C., Cummins L. L., Gonzalez C., Cook P. D. Uniformly modified 2'-deoxy-2'-fluoro phosphorothioate oligonucleotides as nuclease-resistant antisense compounds with high affinity and specificity for RNA targets. J Med Chem. 1993 Apr 2;36(7):831–841. doi: 10.1021/jm00059a007. [DOI] [PubMed] [Google Scholar]
- Kellam P., Boucher C. A., Larder B. A. Fifth mutation in human immunodeficiency virus type 1 reverse transcriptase contributes to the development of high-level resistance to zidovudine. Proc Natl Acad Sci U S A. 1992 Mar 1;89(5):1934–1938. doi: 10.1073/pnas.89.5.1934. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kellam P., Boucher C. A., Tijnagel J. M., Larder B. A. Zidovudine treatment results in the selection of human immunodeficiency virus type 1 variants whose genotypes confer increasing levels of drug resistance. J Gen Virol. 1994 Feb;75(Pt 2):341–351. doi: 10.1099/0022-1317-75-2-341. [DOI] [PubMed] [Google Scholar]
- Kempf D. J., Marsh K. C., Paul D. A., Knigge M. F., Norbeck D. W., Kohlbrenner W. E., Codacovi L., Vasavanonda S., Bryant P., Wang X. C. Antiviral and pharmacokinetic properties of C2 symmetric inhibitors of the human immunodeficiency virus type 1 protease. Antimicrob Agents Chemother. 1991 Nov;35(11):2209–2214. doi: 10.1128/aac.35.11.2209. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kempf D. J., Norbeck D. W., Codacovi L., Wang X. C., Kohlbrenner W. E., Wideburg N. E., Paul D. A., Knigge M. F., Vasavanonda S., Craig-Kennard A. Structure-based, C2 symmetric inhibitors of HIV protease. J Med Chem. 1990 Oct;33(10):2687–2689. doi: 10.1021/jm00172a002. [DOI] [PubMed] [Google Scholar]
- Kleim J. P., Bender R., Billhardt U. M., Meichsner C., Riess G., Rösner M., Winkler I., Paessens A. Activity of a novel quinoxaline derivative against human immunodeficiency virus type 1 reverse transcriptase and viral replication. Antimicrob Agents Chemother. 1993 Aug;37(8):1659–1664. doi: 10.1128/aac.37.8.1659. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kleim J. P., Bender R., Kirsch R., Meichsner C., Paessens A., Riess G. Mutational analysis of residue 190 of human immunodeficiency virus type 1 reverse transcriptase. Virology. 1994 May 1;200(2):696–701. doi: 10.1006/viro.1994.1233. [DOI] [PubMed] [Google Scholar]
- Kleinert H. D., Rosenberg S. H., Baker W. R., Stein H. H., Klinghofer V., Barlow J., Spina K., Polakowski J., Kovar P., Cohen J. Discovery of a peptide-based renin inhibitor with oral bioavailability and efficacy. Science. 1992 Sep 25;257(5078):1940–1943. doi: 10.1126/science.1411510. [DOI] [PubMed] [Google Scholar]
- Kohl N. E., Emini E. A., Schleif W. A., Davis L. J., Heimbach J. C., Dixon R. A., Scolnick E. M., Sigal I. S. Active human immunodeficiency virus protease is required for viral infectivity. Proc Natl Acad Sci U S A. 1988 Jul;85(13):4686–4690. doi: 10.1073/pnas.85.13.4686. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kohlstaedt L. A., Wang J., Friedman J. M., Rice P. A., Steitz T. A. Crystal structure at 3.5 A resolution of HIV-1 reverse transcriptase complexed with an inhibitor. Science. 1992 Jun 26;256(5065):1783–1790. doi: 10.1126/science.1377403. [DOI] [PubMed] [Google Scholar]
- Koizumi N., Sakagami H., Utsumi A., Fujinaga S., Takeda M., Asano K., Sugawara I., Ichikawa S., Kondo H., Mori S. Anti-HIV (human immunodeficiency virus) activity of sulfated paramylon. Antiviral Res. 1993 May;21(1):1–14. doi: 10.1016/0166-3542(93)90063-o. [DOI] [PubMed] [Google Scholar]
- Kong X. B., Zhu Q. Y., Ruprecht R. M., Watanabe K. A., Zeidler J. M., Gold J. W., Polsky B., Armstrong D., Chou T. C. Synergistic inhibition of human immunodeficiency virus type 1 replication in vitro by two-drug and three-drug combinations of 3'-azido-3'-deoxythymidine, phosphonoformate, and 2',3'-dideoxythymidine. Antimicrob Agents Chemother. 1991 Oct;35(10):2003–2011. doi: 10.1128/aac.35.10.2003. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kopp E. B., Miglietta J. J., Shrutkowski A. G., Shih C. K., Grob P. M., Skoog M. T. Steady state kinetics and inhibition of HIV-1 reverse transcriptase by a non-nucleoside dipyridodiazepinone, BI-RG-587, using a heteropolymeric template. Nucleic Acids Res. 1991 Jun 11;19(11):3035–3039. doi: 10.1093/nar/19.11.3035. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kort J. J., Bilello J. A., Bauer G., Drusano G. L. Preclinical evaluation of antiviral activity and toxicity of Abbott A77003, an inhibitor of the human immunodeficiency virus type 1 protease. Antimicrob Agents Chemother. 1993 Jan;37(1):115–119. doi: 10.1128/aac.37.1.115. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Koshida R., Cox S., Harmenberg J., Gilljam G., Wahren B. Structure-activity relationships of fluorinated nucleoside analogs and their synergistic effect in combination with phosphonoformate against human immunodeficiency virus type 1. Antimicrob Agents Chemother. 1989 Dec;33(12):2083–2088. doi: 10.1128/aac.33.12.2083. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Koshida R., Vrang L., Gilljam G., Harmenberg J., Oberg B., Wahren B. Inhibition of human immunodeficiency virus in vitro by combinations of 3'-azido-3'-deoxythymidine and foscarnet. Antimicrob Agents Chemother. 1989 May;33(5):778–780. doi: 10.1128/aac.33.5.778. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Koup R. A., Merluzzi V. J., Hargrave K. D., Adams J., Grozinger K., Eckner R. J., Sullivan J. L. Inhibition of human immunodeficiency virus type 1 (HIV-1) replication by the dipyridodiazepinone BI-RG-587. J Infect Dis. 1991 May;163(5):966–970. doi: 10.1093/infdis/163.5.966. [DOI] [PubMed] [Google Scholar]
- Lacey S. F., Larder B. A. Novel mutation (V75T) in human immunodeficiency virus type 1 reverse transcriptase confers resistance to 2',3'-didehydro-2',3'-dideoxythymidine in cell culture. Antimicrob Agents Chemother. 1994 Jun;38(6):1428–1432. doi: 10.1128/aac.38.6.1428. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Lai M. H., Tang J., Wroblewski V., Dee A. G., Margolin N., Vlahos C., Bowdon B., Buckheit R., Colacino J., Hui K. Y. Impeded progression of Friend disease in mice by an inhibitor of retroviral proteases. J Acquir Immune Defic Syndr. 1993 Jan;6(1):24–31. [PubMed] [Google Scholar]
- Lam P. Y., Jadhav P. K., Eyermann C. J., Hodge C. N., Ru Y., Bacheler L. T., Meek J. L., Otto M. J., Rayner M. M., Wong Y. N. Rational design of potent, bioavailable, nonpeptide cyclic ureas as HIV protease inhibitors. Science. 1994 Jan 21;263(5145):380–384. doi: 10.1126/science.8278812. [DOI] [PubMed] [Google Scholar]
- Lambert D. M., Petteway S. R., Jr, McDanal C. E., Hart T. K., Leary J. J., Dreyer G. B., Meek T. D., Bugelski P. J., Bolognesi D. P., Metcalf B. W. Human immunodeficiency virus type 1 protease inhibitors irreversibly block infectivity of purified virions from chronically infected cells. Antimicrob Agents Chemother. 1992 May;36(5):982–988. doi: 10.1128/aac.36.5.982. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Land S., McGavin C., Lucas R., Birch C. Incidence of zidovudine-resistant human immunodeficiency virus isolated from patients before, during, and after therapy. J Infect Dis. 1992 Nov;166(5):1139–1142. doi: 10.1093/infdis/166.5.1139. [DOI] [PubMed] [Google Scholar]
- Langner K. D., Niedrig M., Fultz P., Anderson D., Reiner G., Repke H., Gelderblom H., Seed B., Hilfenhaus J., Zettlmeissl G. Antiviral effects of different CD4-immunoglobulin constructs against HIV-1 and SIV: immunological characterization, pharmacokinetic data and in vivo experiments. Arch Virol. 1993;130(1-2):157–170. doi: 10.1007/BF01319004. [DOI] [PubMed] [Google Scholar]
- Langtry H. D., Campoli-Richards D. M. Zidovudine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy. Drugs. 1989 Apr;37(4):408–450. doi: 10.2165/00003495-198937040-00003. [DOI] [PubMed] [Google Scholar]
- Larder B. A. 3'-Azido-3'-deoxythymidine resistance suppressed by a mutation conferring human immunodeficiency virus type 1 resistance to nonnucleoside reverse transcriptase inhibitors. Antimicrob Agents Chemother. 1992 Dec;36(12):2664–2669. doi: 10.1128/aac.36.12.2664. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Larder B. A., Coates K. E., Kemp S. D. Zidovudine-resistant human immunodeficiency virus selected by passage in cell culture. J Virol. 1991 Oct;65(10):5232–5236. doi: 10.1128/jvi.65.10.5232-5236.1991. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Larder B. A., Darby G., Richman D. D. HIV with reduced sensitivity to zidovudine (AZT) isolated during prolonged therapy. Science. 1989 Mar 31;243(4899):1731–1734. doi: 10.1126/science.2467383. [DOI] [PubMed] [Google Scholar]
- Larder B. A., Kellam P., Kemp S. D. Convergent combination therapy can select viable multidrug-resistant HIV-1 in vitro. Nature. 1993 Sep 30;365(6445):451–453. doi: 10.1038/365451a0. [DOI] [PubMed] [Google Scholar]
- Larder B. A., Kemp S. D. Multiple mutations in HIV-1 reverse transcriptase confer high-level resistance to zidovudine (AZT). Science. 1989 Dec 1;246(4934):1155–1158. doi: 10.1126/science.2479983. [DOI] [PubMed] [Google Scholar]
- Lasarte J. J., Sarobe P., Golvano J., Prieto I., Civeira M. P., Gullón A., Sarin P. S., Prieto J., Borrás-Cuesta F. CD4-modified synthetic peptides containing phenylalanine inhibit HIV-1 infection in vitro. J Acquir Immune Defic Syndr. 1994 Feb;7(2):129–134. [PubMed] [Google Scholar]
- Lavie G., Valentine F., Levin B., Mazur Y., Gallo G., Lavie D., Weiner D., Meruelo D. Studies of the mechanisms of action of the antiretroviral agents hypericin and pseudohypericin. Proc Natl Acad Sci U S A. 1989 Aug;86(15):5963–5967. doi: 10.1073/pnas.86.15.5963. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Lee-Huang S., Huang P. L., Kung H. F., Li B. Q., Huang P. L., Huang P., Huang H. I., Chen H. C. TAP 29: an anti-human immunodeficiency virus protein from Trichosanthes kirilowii that is nontoxic to intact cells. Proc Natl Acad Sci U S A. 1991 Aug 1;88(15):6570–6574. doi: 10.1073/pnas.88.15.6570. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Lenard J., Rabson A., Vanderoef R. Photodynamic inactivation of infectivity of human immunodeficiency virus and other enveloped viruses using hypericin and rose bengal: inhibition of fusion and syncytia formation. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):158–162. doi: 10.1073/pnas.90.1.158. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Li C. J., Zhang L. J., Dezube B. J., Crumpacker C. S., Pardee A. B. Three inhibitors of type 1 human immunodeficiency virus long terminal repeat-directed gene expression and virus replication. Proc Natl Acad Sci U S A. 1993 Mar 1;90(5):1839–1842. doi: 10.1073/pnas.90.5.1839. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Lin T. S., Luo M. Z., Liu M. C., Pai S. B., Dutschman G. E., Cheng Y. C. Antiviral activity of 2',3'-dideoxy-beta-L-5-fluorocytidine (beta-L-FddC) and 2',3'-dideoxy-beta-L-cytidine (beta-L-ddC) against hepatitis B virus and human immunodeficiency virus type 1 in vitro. Biochem Pharmacol. 1994 Jan 20;47(2):171–174. doi: 10.1016/0006-2952(94)90002-7. [DOI] [PubMed] [Google Scholar]
- Lin T. S., Schinazi R. F., Chen M. S., Kinney-Thomas E., Prusoff W. H. Antiviral activity of 2',3'-dideoxycytidin-2'-ene (2',3'-dideoxy-2',3'-didehydrocytidine) against human immunodeficiency virus in vitro. Biochem Pharmacol. 1987 Feb 1;36(3):311–316. doi: 10.1016/0006-2952(87)90287-5. [DOI] [PubMed] [Google Scholar]
- Lin T. S., Schinazi R. F., Prusoff W. H. Potent and selective in vitro activity of 3'-deoxythymidin-2'-ene (3'-deoxy-2',3'-didehydrothymidine) against human immunodeficiency virus. Biochem Pharmacol. 1987 Sep 1;36(17):2713–2718. doi: 10.1016/0006-2952(87)90253-x. [DOI] [PubMed] [Google Scholar]
- Lin T. S., Schinazi R. F., Zhu J., Birks E., Carbone R., Si Y., Wu K., Huang L., Prusoff W. H. Anti-HIV-1 activity and cellular pharmacology of various analogs of gossypol. Biochem Pharmacol. 1993 Jul 20;46(2):251–255. doi: 10.1016/0006-2952(93)90411-o. [DOI] [PubMed] [Google Scholar]
- Lin T. S., Schinazi R., Griffith B. P., August E. M., Eriksson B. F., Zheng D. K., Huang L. A., Prusoff W. H. Selective inhibition of human immunodeficiency virus type 1 replication by the (-) but not the (+) enantiomer of gossypol. Antimicrob Agents Chemother. 1989 Dec;33(12):2149–2151. doi: 10.1128/aac.33.12.2149. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Lisziewicz J., Sun D., Klotman M., Agrawal S., Zamecnik P., Gallo R. Specific inhibition of human immunodeficiency virus type 1 replication by antisense oligonucleotides: an in vitro model for treatment. Proc Natl Acad Sci U S A. 1992 Dec 1;89(23):11209–11213. doi: 10.1073/pnas.89.23.11209. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Livermore D. G., Bethell R. C., Cammack N., Hancock A. P., Hann M. M., Green D. V., Lamont R. B., Noble S. A., Orr D. C., Payne J. J. Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines. J Med Chem. 1993 Nov 26;36(24):3784–3794. doi: 10.1021/jm00076a005. [DOI] [PubMed] [Google Scholar]
- Lo K. M., Biasolo M. A., Dehni G., Palú G., Haseltine W. A. Inhibition of replication of HIV-1 by retroviral vectors expressing tat-antisense and anti-tat ribozyme RNA. Virology. 1992 Sep;190(1):176–183. doi: 10.1016/0042-6822(92)91203-7. [DOI] [PubMed] [Google Scholar]
- Lorentsen K. J., Hendrix C. W., Collins J. M., Kornhauser D. M., Petty B. G., Klecker R. W., Flexner C., Eckel R. H., Lietman P. S. Dextran sulfate is poorly absorbed after oral administration. Ann Intern Med. 1989 Oct 1;111(7):561–566. doi: 10.7326/0003-4819-111-7-561. [DOI] [PubMed] [Google Scholar]
- Lori F., Malykh A., Cara A., Sun D., Weinstein J. N., Lisziewicz J., Gallo R. C. Hydroxyurea as an inhibitor of human immunodeficiency virus-type 1 replication. Science. 1994 Nov 4;266(5186):801–805. doi: 10.1126/science.7973634. [DOI] [PubMed] [Google Scholar]
- Loya S., Hizi A. The inhibition of human immunodeficiency virus type 1 reverse transcriptase by avarol and avarone derivatives. FEBS Lett. 1990 Aug 20;269(1):131–134. doi: 10.1016/0014-5793(90)81137-d. [DOI] [PubMed] [Google Scholar]
- Loya S., Hizi A. The interaction of illimaquinone, a selective inhibitor of the RNase H activity, with the reverse transcriptases of human immunodeficiency and murine leukemia retroviruses. J Biol Chem. 1993 May 5;268(13):9323–9328. [PubMed] [Google Scholar]
- Loya S., Tal R., Kashman Y., Hizi A. Illimaquinone, a selective inhibitor of the RNase H activity of human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1990 Oct;34(10):2009–2012. doi: 10.1128/aac.34.10.2009. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Lyle T. A., Wiscount C. M., Guare J. P., Thompson W. J., Anderson P. S., Darke P. L., Zugay Z. A., Emini E. A., Schleif W. A., Qunitero J. C. Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors. J Med Chem. 1991 Mar;34(3):1228–1230. doi: 10.1021/jm00107a051. [DOI] [PubMed] [Google Scholar]
- Lynch G., Low L., Li S., Sloane A., Adams S., Parish C., Kemp B., Cunningham A. L. Sulfated polyanions prevent HIV infection of lymphocytes by disruption of the CD4-gp120 interaction, but do not inhibit monocyte infection. J Leukoc Biol. 1994 Sep;56(3):266–272. doi: 10.1002/jlb.56.3.266. [DOI] [PubMed] [Google Scholar]
- Maag H., Nelson J. T., Steiner J. L., Prisbe E. J. Solid-state and solution conformations of the potent HIV inhibitor, 4'-azidothymidine. J Med Chem. 1994 Feb 18;37(4):431–438. doi: 10.1021/jm00030a001. [DOI] [PubMed] [Google Scholar]
- Maass G., Immendoerfer U., Koenig B., Leser U., Mueller B., Goody R., Pfaff E. Viral resistance to the thiazolo-iso-indolinones, a new class of nonnucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1993 Dec;37(12):2612–2617. doi: 10.1128/aac.37.12.2612. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Mahmood N., Pizza C., Aquino R., De Tommasi N., Piacente S., Colman S., Burke A., Hay A. J. Inhibition of HIV infection by flavanoids. Antiviral Res. 1993 Oct;22(2-3):189–199. doi: 10.1016/0166-3542(93)90095-z. [DOI] [PubMed] [Google Scholar]
- Mahoney C. W., Azzi A., Huang K. P. Effects of suramin, an anti-human immunodeficiency virus reverse transcriptase agent, on protein kinase C. Differential activation and inhibition of protein kinase C isozymes. J Biol Chem. 1990 Apr 5;265(10):5424–5428. [PubMed] [Google Scholar]
- Malley S. D., Grange J. M., Hamedi-Sangsari F., Vila J. R. Synergistic anti-human immunodeficiency virus type 1 effect of hydroxamate compounds with 2',3'-dideoxyinosine in infected resting human lymphocytes. Proc Natl Acad Sci U S A. 1994 Nov 8;91(23):11017–11021. doi: 10.1073/pnas.91.23.11017. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Margolis D. M., Ostrove J. M., Straus S. E. HSV-1 activation of HIV-1 transcription is augmented by a cellular protein that binds near the initiator element. Virology. 1993 Jan;192(1):370–374. doi: 10.1006/viro.1993.1046. [DOI] [PubMed] [Google Scholar]
- Marshall W. S., Caruthers M. H. Phosphorodithioate DNA as a potential therapeutic drug. Science. 1993 Mar 12;259(5101):1564–1570. doi: 10.1126/science.7681216. [DOI] [PubMed] [Google Scholar]
- Mathes L. E., Hayes K. A., Swenson C. L., Polas P. J., Weisbrode S. E., Kociba G. J. Evaluation of antiviral activity and toxicity of dextran sulfate in feline leukemia virus-infected cats. Antimicrob Agents Chemother. 1991 Oct;35(10):2147–2150. doi: 10.1128/aac.35.10.2147. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Matsui T., Kobayashi S., Yoshida O., Ishii S., Abe Y., Yamamoto N. Effects of succinylated concanavalin A on infectivity and syncytial formation of human immunodeficiency virus. Med Microbiol Immunol. 1990;179(5):225–235. doi: 10.1007/BF00192460. [DOI] [PubMed] [Google Scholar]
- Matsukura M., Shinozuka K., Zon G., Mitsuya H., Reitz M., Cohen J. S., Broder S. Phosphorothioate analogs of oligodeoxynucleotides: inhibitors of replication and cytopathic effects of human immunodeficiency virus. Proc Natl Acad Sci U S A. 1987 Nov;84(21):7706–7710. doi: 10.1073/pnas.84.21.7706. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Matsukura M., Zon G., Shinozuka K., Robert-Guroff M., Shimada T., Stein C. A., Mitsuya H., Wong-Staal F., Cohen J. S., Broder S. Regulation of viral expression of human immunodeficiency virus in vitro by an antisense phosphorothioate oligodeoxynucleotide against rev (art/trs) in chronically infected cells. Proc Natl Acad Sci U S A. 1989 Jun;86(11):4244–4248. doi: 10.1073/pnas.86.11.4244. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Mayaux J. F., Bousseau A., Pauwels R., Huet T., Hénin Y., Dereu N., Evers M., Soler F., Poujade C., De Clercq E. Triterpene derivatives that block entry of human immunodeficiency virus type 1 into cells. Proc Natl Acad Sci U S A. 1994 Apr 26;91(9):3564–3568. doi: 10.1073/pnas.91.9.3564. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Mayers D. L., Japour A. J., Arduino J. M., Hammer S. M., Reichman R., Wagner K. F., Chung R., Lane J., Crumpacker C. S., McLeod G. X. Dideoxynucleoside resistance emerges with prolonged zidovudine monotherapy. The RV43 Study Group. Antimicrob Agents Chemother. 1994 Feb;38(2):307–314. doi: 10.1128/aac.38.2.307. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Mayers D. L., McCutchan F. E., Sanders-Buell E. E., Merritt L. I., Dilworth S., Fowler A. K., Marks C. A., Ruiz N. M., Richman D. D., Roberts C. R. Characterization of HIV isolates arising after prolonged zidovudine therapy. J Acquir Immune Defic Syndr. 1992;5(8):749–759. [PubMed] [Google Scholar]
- Mazzulli T., Rusconi S., Merrill D. P., D'Aquila R. T., Moonis M., Chou T. C., Hirsch M. S. Alternating versus continuous drug regimens in combination chemotherapy of human immunodeficiency virus type 1 infection in vitro. Antimicrob Agents Chemother. 1994 Apr;38(4):656–661. doi: 10.1128/aac.38.4.656. [DOI] [PMC free article] [PubMed] [Google Scholar]
- McGrath M. S., Hwang K. M., Caldwell S. E., Gaston I., Luk K. C., Wu P., Ng V. L., Crowe S., Daniels J., Marsh J. GLQ223: an inhibitor of human immunodeficiency virus replication in acutely and chronically infected cells of lymphocyte and mononuclear phagocyte lineage. Proc Natl Acad Sci U S A. 1989 Apr;86(8):2844–2848. doi: 10.1073/pnas.86.8.2844. [DOI] [PMC free article] [PubMed] [Google Scholar]
- McGuigan C., Pathirana R. N., Balzarini J., De Clercq E. Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT. J Med Chem. 1993 Apr 16;36(8):1048–1052. doi: 10.1021/jm00060a013. [DOI] [PubMed] [Google Scholar]
- McMahon J. B., Gulakowski R. J., Weislow O. S., Schultz R. J., Narayanan V. L., Clanton D. J., Pedemonte R., Wassmundt F. W., Buckheit R. W., Jr, Decker W. D. Diarylsulfones, a new chemical class of nonnucleoside antiviral inhibitors of human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1993 Apr;37(4):754–760. doi: 10.1128/aac.37.4.754. [DOI] [PMC free article] [PubMed] [Google Scholar]
- McQuade T. J., Tomasselli A. G., Liu L., Karacostas V., Moss B., Sawyer T. K., Heinrikson R. L., Tarpley W. G. A synthetic HIV-1 protease inhibitor with antiviral activity arrests HIV-like particle maturation. Science. 1990 Jan 26;247(4941):454–456. doi: 10.1126/science.2405486. [DOI] [PubMed] [Google Scholar]
- McShan W. M., Rossen R. D., Laughter A. H., Trial J., Kessler D. J., Zendegui J. G., Hogan M. E., Orson F. M. Inhibition of transcription of HIV-1 in infected human cells by oligodeoxynucleotides designed to form DNA triple helices. J Biol Chem. 1992 Mar 15;267(8):5712–5721. [PubMed] [Google Scholar]
- Medina D. J., Hsiung G. D., Mellors J. W. Ganciclovir antagonizes the anti-human immunodeficiency virus type 1 activity of zidovudine and didanosine in vitro. Antimicrob Agents Chemother. 1992 May;36(5):1127–1130. doi: 10.1128/aac.36.5.1127. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Mellors J. W., Dutschman G. E., Im G. J., Tramontano E., Winkler S. R., Cheng Y. C. In vitro selection and molecular characterization of human immunodeficiency virus-1 resistant to non-nucleoside inhibitors of reverse transcriptase. Mol Pharmacol. 1992 Mar;41(3):446–451. [PubMed] [Google Scholar]
- Mellors J. W., Im G. J., Tramontano E., Winkler S. R., Medina D. J., Dutschman G. E., Bazmi H. Z., Piras G., Gonzalez C. J., Cheng Y. C. A single conservative amino acid substitution in the reverse transcriptase of human immunodeficiency virus-1 confers resistance to (+)-(5S)-4,5,6,7-tetrahydro-5-methyl-6-(3-methyl-2-butenyl)imidazo[4,5, 1- jk][1,4]benzodiazepin-2(1H)-thione (TIBO R82150). Mol Pharmacol. 1993 Jan;43(1):11–16. [PubMed] [Google Scholar]
- Meng T. C., Fischl M. A., Boota A. M., Spector S. A., Bennett D., Bassiakos Y., Lai S. H., Wright B., Richman D. D. Combination therapy with zidovudine and dideoxycytidine in patients with advanced human immunodeficiency virus infection. A phase I/II study. Ann Intern Med. 1992 Jan 1;116(1):13–20. doi: 10.7326/0003-4819-116-1-13. [DOI] [PubMed] [Google Scholar]
- Mergny J. L., Duval-Valentin G., Nguyen C. H., Perrouault L., Faucon B., Rougée M., Montenay-Garestier T., Bisagni E., Hélène C. Triple helix-specific ligands. Science. 1992 Jun 19;256(5064):1681–1684. doi: 10.1126/science.256.5064.1681. [DOI] [PubMed] [Google Scholar]
- Merluzzi V. J., Hargrave K. D., Labadia M., Grozinger K., Skoog M., Wu J. C., Shih C. K., Eckner K., Hattox S., Adams J. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science. 1990 Dec 7;250(4986):1411–1413. doi: 10.1126/science.1701568. [DOI] [PubMed] [Google Scholar]
- Mertens A., Zilch H., König B., Schäfer W., Poll T., Kampe W., Seidel H., Leser U., Leinert H. Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity. J Med Chem. 1993 Aug 20;36(17):2526–2535. doi: 10.1021/jm00069a011. [DOI] [PubMed] [Google Scholar]
- Meruelo D., Lavie G., Lavie D. Therapeutic agents with dramatic antiretroviral activity and little toxicity at effective doses: aromatic polycyclic diones hypericin and pseudohypericin. Proc Natl Acad Sci U S A. 1988 Jul;85(14):5230–5234. doi: 10.1073/pnas.85.14.5230. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Meylan P. R., Guatelli J. C., Munis J. R., Richman D. D., Kornbluth R. S. Mechanisms for the inhibition of HIV replication by interferons-alpha, -beta, and -gamma in primary human macrophages. Virology. 1993 Mar;193(1):138–148. doi: 10.1006/viro.1993.1110. [DOI] [PubMed] [Google Scholar]
- Michne W. F., Schroeder J. D., Bailey T. R., Young D. C., Hughes J. V., Dutko F. J. Keto/enol epoxy steroids: a new structural class of HIV-1 Tat inhibitors. J Med Chem. 1993 Sep 3;36(18):2701–2702. doi: 10.1021/jm00070a014. [DOI] [PubMed] [Google Scholar]
- Milligan J. F., Matteucci M. D., Martin J. C. Current concepts in antisense drug design. J Med Chem. 1993 Jul 9;36(14):1923–1937. doi: 10.1021/jm00066a001. [DOI] [PubMed] [Google Scholar]
- Mitsuya H., Broder S. Inhibition of the in vitro infectivity and cytopathic effect of human T-lymphotrophic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV) by 2',3'-dideoxynucleosides. Proc Natl Acad Sci U S A. 1986 Mar;83(6):1911–1915. doi: 10.1073/pnas.83.6.1911. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Mitsuya H., Broder S. Strategies for antiviral therapy in AIDS. 1987 Feb 26-Mar 4Nature. 325(6107):773–778. doi: 10.1038/325773a0. [DOI] [PubMed] [Google Scholar]
- Mitsuya H., Popovic M., Yarchoan R., Matsushita S., Gallo R. C., Broder S. Suramin protection of T cells in vitro against infectivity and cytopathic effect of HTLV-III. Science. 1984 Oct 12;226(4671):172–174. doi: 10.1126/science.6091268. [DOI] [PubMed] [Google Scholar]
- Mitsuya H., Weinhold K. J., Furman P. A., St Clair M. H., Lehrman S. N., Gallo R. C., Bolognesi D., Barry D. W., Broder S. 3'-Azido-3'-deoxythymidine (BW A509U): an antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro. Proc Natl Acad Sci U S A. 1985 Oct;82(20):7096–7100. doi: 10.1073/pnas.82.20.7096. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Mitsuya H., Yarchoan R., Broder S. Molecular targets for AIDS therapy. Science. 1990 Sep 28;249(4976):1533–1544. doi: 10.1126/science.1699273. [DOI] [PubMed] [Google Scholar]
- Miyasaka T., Tanaka H., Baba M., Hayakawa H., Walker R. T., Balzarini J., De Clercq E. A novel lead for specific anti-HIV-1 agents: 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. J Med Chem. 1989 Dec;32(12):2507–2509. doi: 10.1021/jm00132a002. [DOI] [PubMed] [Google Scholar]
- Moelling K., Schulze T., Diringer H. Inhibition of human immunodeficiency virus type 1 RNase H by sulfated polyanions. J Virol. 1989 Dec;63(12):5489–5491. doi: 10.1128/jvi.63.12.5489-5491.1989. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Mohan P., Loya S., Avidan O., Verma S., Dhindsa G. S., Wong M. F., Huang P. P., Yashiro M., Baba M., Hizi A. Synthesis of naphthalenesulfonic acid small molecules as selective inhibitors of the DNA polymerase and ribonuclease H activities of HIV-1 reverse transcriptase. J Med Chem. 1994 Aug 5;37(16):2513–2519. doi: 10.1021/jm00042a004. [DOI] [PubMed] [Google Scholar]
- Mohan P., Schols D., Baba M., De Clercq E. Sulfonic acid polymers as a new class of human immunodeficiency virus inhibitors. Antiviral Res. 1992 Jun;18(2):139–150. doi: 10.1016/0166-3542(92)90034-3. [DOI] [PubMed] [Google Scholar]
- Mohan P., Singh R., Baba M. Anti-HIV-1 and HIV-2 activity of naphthalenedisulfonic acid derivatives. Inhibition of cytopathogenesis, giant cell formation, and reverse transcriptase activity. Biochem Pharmacol. 1991 Feb 15;41(4):642–646. doi: 10.1016/0006-2952(91)90641-h. [DOI] [PubMed] [Google Scholar]
- Mohan P., Singh R., Baba M. Potential anti-AIDS agents. Synthesis and antiviral activity of naphthalenesulfonic acid derivatives against HIV-1 and HIV-2. J Med Chem. 1991 Jan;34(1):212–217. doi: 10.1021/jm00105a033. [DOI] [PubMed] [Google Scholar]
- Mohan P., Singh R., Wepsiec J., Gonzalez I., Sun D. K., Sarin P. S. Inhibition of HIV replication by naphthalenemonosulfonic acid derivatives and a bis naphthalenedisulfonic acid compound. Life Sci. 1990;47(12):993–999. doi: 10.1016/0024-3205(90)90471-3. [DOI] [PubMed] [Google Scholar]
- Mohan P., Wong M. F., Verma S., Huang P. P., Wickramasinghe A., Baba M. Structure-activity relationship studies with symmetric naphthalenesulfonic acid derivatives. Synthesis and influence of spacer and naphthalenesulfonic acid moiety on anti-HIV-1 activity. J Med Chem. 1993 Jul 9;36(14):1996–2003. doi: 10.1021/jm00066a008. [DOI] [PubMed] [Google Scholar]
- Mohri H., Singh M. K., Ching W. T., Ho D. D. Quantitation of zidovudine-resistant human immunodeficiency virus type 1 in the blood of treated and untreated patients. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):25–29. doi: 10.1073/pnas.90.1.25. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Montefiori D. C., Robinson W. E., Jr, Mitchell W. M. Role of protein N-glycosylation in pathogenesis of human immunodeficiency virus type 1. Proc Natl Acad Sci U S A. 1988 Dec;85(23):9248–9252. doi: 10.1073/pnas.85.23.9248. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Moriya T., Kurita H., Matsumoto K., Otake T., Mori H., Morimoto M., Ueba N., Kunita N. Potent inhibitory effect of a series of modified cyclodextrin sulfates (mCDS) on the replication of HIV-1 in vitro. J Med Chem. 1991 Jul;34(7):2301–2304. doi: 10.1021/jm00111a055. [DOI] [PubMed] [Google Scholar]
- Moriya T., Saito K., Kurita H., Matsumoto K., Otake T., Mori H., Morimoto M., Ueba N., Kunita N. A new candidate for an anti-HIV-1 agent: modified cyclodextrin sulfate (mCDS71). J Med Chem. 1993 May 28;36(11):1674–1677. doi: 10.1021/jm00063a018. [DOI] [PubMed] [Google Scholar]
- Müller W. E., Renneisen K., Kreuter M. H., Schröder H. C., Winkler I. The D-mannose-specific lectin from Gerardia savaglia blocks binding of human immunodeficiency virus type I to H9 cells and human lymphocytes in vitro. J Acquir Immune Defic Syndr. 1988;1(5):453–458. [PubMed] [Google Scholar]
- Müller W. E., Weiler B. E., Charubala R., Pfleiderer W., Leserman L., Sobol R. W., Suhadolnik R. J., Schröder H. C. Cordycepin analogues of 2',5'-oligoadenylate inhibit human immunodeficiency virus infection via inhibition of reverse transcriptase. Biochemistry. 1991 Feb 26;30(8):2027–2033. doi: 10.1021/bi00222a004. [DOI] [PubMed] [Google Scholar]
- Naesens L., Balzarini J., De Clercq E. Single-dose administration of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) and 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) in the prophylaxis of retrovirus infection in vivo. Antiviral Res. 1991 Jul;16(1):53–64. doi: 10.1016/0166-3542(91)90058-y. [DOI] [PubMed] [Google Scholar]
- Nakamura S., Sakurada S., Salahuddin S. Z., Osada Y., Tanaka N. G., Sakamoto N., Sekiguchi M., Gallo R. C. Inhibition of development of Kaposi's sarcoma-related lesions by a bacterial cell wall complex. Science. 1992 Mar 13;255(5050):1437–1440. doi: 10.1126/science.1371891. [DOI] [PubMed] [Google Scholar]
- Nakane H., Arisawa M., Fujita A., Koshimura S., Ono K. Inhibition of HIV-reverse transcriptase activity by some phloroglucinol derivatives. FEBS Lett. 1991 Jul 29;286(1-2):83–85. doi: 10.1016/0014-5793(91)80946-z. [DOI] [PubMed] [Google Scholar]
- Nakane H., Ono K. Differential inhibitory effects of some catechin derivatives on the activities of human immunodeficiency virus reverse transcriptase and cellular deoxyribonucleic and ribonucleic acid polymerases. Biochemistry. 1990 Mar 20;29(11):2841–2845. doi: 10.1021/bi00463a029. [DOI] [PubMed] [Google Scholar]
- Nakashima H., Masuda M., Murakami T., Koyanagi Y., Matsumoto A., Fujii N., Yamamoto N. Anti-human immunodeficiency virus activity of a novel synthetic peptide, T22 ([Tyr-5,12, Lys-7]polyphemusin II): a possible inhibitor of virus-cell fusion. Antimicrob Agents Chemother. 1992 Jun;36(6):1249–1255. doi: 10.1128/aac.36.6.1249. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Nakashima H., Matsui T., Yoshida O., Isowa Y., Kido Y., Motoki Y., Ito M., Shigeta S., Mori T., Yamamoto N. A new anti-human immunodeficiency virus substance, glycyrrhizin sulfate; endowment of glycyrrhizin with reverse transcriptase-inhibitory activity by chemical modification. Jpn J Cancer Res. 1987 Aug;78(8):767–771. [PubMed] [Google Scholar]
- Nasr M., Litterst C., McGowan J. Computer-assisted structure-activity correlations of dideoxynucleoside analogs as potential anti-HIV drugs. Antiviral Res. 1990 Sep;14(3):125–148. doi: 10.1016/0166-3542(90)90030-b. [DOI] [PubMed] [Google Scholar]
- Navia M. A., Fitzgerald P. M., McKeever B. M., Leu C. T., Heimbach J. C., Herber W. K., Sigal I. S., Darke P. L., Springer J. P. Three-dimensional structure of aspartyl protease from human immunodeficiency virus HIV-1. Nature. 1989 Feb 16;337(6208):615–620. doi: 10.1038/337615a0. [DOI] [PubMed] [Google Scholar]
- Newlander K. A., Callahan J. F., Moore M. L., Tomaszek T. A., Jr, Huffman W. F. A novel constrained reduced-amide inhibitor of HIV-1 protease derived from the sequential incorporation of gamma-turn mimetics into a model substrate. J Med Chem. 1993 Aug 6;36(16):2321–2331. doi: 10.1021/jm00068a008. [DOI] [PubMed] [Google Scholar]
- Nozaki-Renard J., Iino T., Sato Y., Marumoto Y., Ohta G., Furusawa M. Fluoroquinolones protect the human lymphocyte CEM cell line from HIV-1-mediated cytotoxicity. Cell Struct Funct. 1990 Oct;15(5):295–299. doi: 10.1247/csf.15.295. [DOI] [PubMed] [Google Scholar]
- Nunberg J. H., Schleif W. A., Boots E. J., O'Brien J. A., Quintero J. C., Hoffman J. M., Emini E. A., Goldman M. E. Viral resistance to human immunodeficiency virus type 1-specific pyridinone reverse transcriptase inhibitors. J Virol. 1991 Sep;65(9):4887–4892. doi: 10.1128/jvi.65.9.4887-4892.1991. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Offensperger W. B., Offensperger S., Walter E., Blum H. E., Gerok W. Sulfated polyanions do not inhibit duck hepatitis B virus infection. Antimicrob Agents Chemother. 1991 Nov;35(11):2431–2433. doi: 10.1128/aac.35.11.2431. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Ojwang J., Elbaggari A., Marshall H. B., Jayaraman K., McGrath M. S., Rando R. F. Inhibition of human immunodeficiency virus type 1 activity in vitro by oligonucleotides composed entirely of guanosine and thymidine. J Acquir Immune Defic Syndr. 1994 Jun;7(6):560–570. [PubMed] [Google Scholar]
- Okada T., Patterson B. K., Ye S. Q., Gurney M. E. Aurothiolates inhibit HIV-1 infectivity by gold(I) ligand exchange with a component of the virion surface. Virology. 1993 Feb;192(2):631–642. doi: 10.1006/viro.1993.1079. [DOI] [PubMed] [Google Scholar]
- Otake T., Miyano K., Mori H., Morimoto M., Ueba N., Kunita N., Nakashima H., Kurimura T. Anti-HIV-1 activity of sulfated amphotericin B in vitro. Antiviral Res. 1991 Oct;16(3):243–255. doi: 10.1016/0166-3542(91)90004-b. [DOI] [PubMed] [Google Scholar]
- Otto M. J., Garber S., Winslow D. L., Reid C. D., Aldrich P., Jadhav P. K., Patterson C. E., Hodge C. N., Cheng Y. S. In vitro isolation and identification of human immunodeficiency virus (HIV) variants with reduced sensitivity to C-2 symmetrical inhibitors of HIV type 1 protease. Proc Natl Acad Sci U S A. 1993 Aug 15;90(16):7543–7547. doi: 10.1073/pnas.90.16.7543. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Otto M. J., Reid C. D., Garber S., Lam P. Y., Scarnati H., Bacheler L. T., Rayner M. M., Winslow D. L. In vitro anti-human immunodeficiency virus (HIV) activity of XM323, a novel HIV protease inhibitor. Antimicrob Agents Chemother. 1993 Dec;37(12):2606–2611. doi: 10.1128/aac.37.12.2606. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Pal R., Kalyanaraman V. S., Hoke G. M., Sarngadharan M. G. Processing and secretion of envelope glycoproteins of human immunodeficiency virus type 1 in the presence of trimming glucosidase inhibitor deoxynojirimycin. Intervirology. 1989;30(1):27–35. doi: 10.1159/000150073. [DOI] [PubMed] [Google Scholar]
- Pal R., Mumbauer S., Hoke G., Larocca R., Myers C., Sarngadharan M. G., Stein C. A. Effect of Evans blue and trypan blue on syncytia formation and infectivity of human immunodeficiency virus type I and type II in vitro. AIDS Res Hum Retroviruses. 1991 Jun;7(6):537–543. doi: 10.1089/aid.1991.7.537. [DOI] [PubMed] [Google Scholar]
- Patel M., Yanagishita M., Roderiquez G., Bou-Habib D. C., Oravecz T., Hascall V. C., Norcross M. A. Cell-surface heparan sulfate proteoglycan mediates HIV-1 infection of T-cell lines. AIDS Res Hum Retroviruses. 1993 Feb;9(2):167–174. doi: 10.1089/aid.1993.9.167. [DOI] [PubMed] [Google Scholar]
- Patil A. D., Freyer A. J., Eggleston D. S., Haltiwanger R. C., Bean M. F., Taylor P. B., Caranfa M. J., Breen A. L., Bartus H. R., Johnson R. K. The inophyllums, novel inhibitors of HIV-1 reverse transcriptase isolated from the Malaysian tree, Calophyllum inophyllum Linn. J Med Chem. 1993 Dec 24;36(26):4131–4138. doi: 10.1021/jm00078a001. [DOI] [PubMed] [Google Scholar]
- Pauwels R., Andries K., Debyser Z., Van Daele P., Schols D., Stoffels P., De Vreese K., Woestenborghs R., Vandamme A. M., Janssen C. G. Potent and highly selective human immunodeficiency virus type 1 (HIV-1) inhibition by a series of alpha-anilinophenylacetamide derivatives targeted at HIV-1 reverse transcriptase. Proc Natl Acad Sci U S A. 1993 Mar 1;90(5):1711–1715. doi: 10.1073/pnas.90.5.1711. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Pauwels R., Andries K., Desmyter J., Schols D., Kukla M. J., Breslin H. J., Raeymaeckers A., Van Gelder J., Woestenborghs R., Heykants J. Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives. Nature. 1990 Feb 1;343(6257):470–474. doi: 10.1038/343470a0. [DOI] [PubMed] [Google Scholar]
- Pauwels R., Balzarini J., Schols D., Baba M., Desmyter J., Rosenberg I., Holy A., De Clercq E. Phosphonylmethoxyethyl purine derivatives, a new class of anti-human immunodeficiency virus agents. Antimicrob Agents Chemother. 1988 Jul;32(7):1025–1030. doi: 10.1128/aac.32.7.1025. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Peters M., Witvrouw M., De Clercq E., Ruf B. Pharmacokinetics of intravenous pentosan polysulphate (HOE/BAY 946) in HIV-positive patients. AIDS. 1991 Dec;5(12):1534–1535. doi: 10.1097/00002030-199112000-00021. [DOI] [PubMed] [Google Scholar]
- Pialoux G., Youle M., Dupont B., Gazzard B., Cauwenbergh G. F., Stoffels P. A., Davies S., de Saint Martin J., Janssen P. A. Pharmacokinetics of R 82913 in patients with AIDS or AIDS-related complex. Lancet. 1991 Jul 20;338(8760):140–143. doi: 10.1016/0140-6736(91)90135-c. [DOI] [PubMed] [Google Scholar]
- Pieken W. A., Olsen D. B., Benseler F., Aurup H., Eckstein F. Kinetic characterization of ribonuclease-resistant 2'-modified hammerhead ribozymes. Science. 1991 Jul 19;253(5017):314–317. doi: 10.1126/science.1857967. [DOI] [PubMed] [Google Scholar]
- Pluda J. M., Shay L. E., Foli A., Tannenbaum S., Cohen P. J., Goldspiel B. R., Adamo D., Cooper M. R., Broder S., Yarchoan R. Administration of pentosan polysulfate to patients with human immunodeficiency virus-associated Kaposi's sarcoma. J Natl Cancer Inst. 1993 Oct 6;85(19):1585–1592. doi: 10.1093/jnci/85.19.1585. [DOI] [PubMed] [Google Scholar]
- Poli G., Orenstein J. M., Kinter A., Folks T. M., Fauci A. S. Interferon-alpha but not AZT suppresses HIV expression in chronically infected cell lines. Science. 1989 May 5;244(4904):575–577. doi: 10.1126/science.2470148. [DOI] [PubMed] [Google Scholar]
- Popik W., Pitha P. M. Transcriptional activation of the tat-defective human immunodeficiency virus type-1 provirus: effect of interferon. Virology. 1992 Aug;189(2):435–447. doi: 10.1016/0042-6822(92)90567-9. [DOI] [PubMed] [Google Scholar]
- Prochaska H. J., Yeh Y., Baron P., Polsky B. Oltipraz, an inhibitor of human immunodeficiency virus type 1 replication. Proc Natl Acad Sci U S A. 1993 May 1;90(9):3953–3957. doi: 10.1073/pnas.90.9.3953. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Puech F., Gosselin G., Lefebvre I., Pompon A., Aubertin A. M., Kirn A., Imbach J. L. Intracellular delivery of nucleoside monophosphates through a reductase-mediated activation process. Antiviral Res. 1993 Oct;22(2-3):155–174. doi: 10.1016/0166-3542(93)90093-x. [DOI] [PubMed] [Google Scholar]
- Puglisi J. D., Tan R., Calnan B. J., Frankel A. D., Williamson J. R. Conformation of the TAR RNA-arginine complex by NMR spectroscopy. Science. 1992 Jul 3;257(5066):76–80. doi: 10.1126/science.1621097. [DOI] [PubMed] [Google Scholar]
- Pulliam L., Herndier B. G., McGrath M. S. Purified trichosanthin (GLQ223) exacerbation of indirect HIV-associated neurotoxicity in vitro. AIDS. 1991 Oct;5(10):1237–1242. doi: 10.1097/00002030-199110000-00013. [DOI] [PubMed] [Google Scholar]
- Pätzold S., Schneider J., Rudolph C., Marmé D., Schächtele C. Novel indolocarbazole protein kinase C inhibitors prevent reactivation of HIV-1 in latently infected cells. Antiviral Res. 1993 Dec;22(4):273–283. doi: 10.1016/0166-3542(93)90037-j. [DOI] [PubMed] [Google Scholar]
- Qatsha K. A., Rudolph C., Marmé D., Schächtele C., May W. S. Gö 6976, a selective inhibitor of protein kinase C, is a potent antagonist of human immunodeficiency virus 1 induction from latent/low-level-producing reservoir cells in vitro. Proc Natl Acad Sci U S A. 1993 May 15;90(10):4674–4678. doi: 10.1073/pnas.90.10.4674. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Ratner L., vander Heyden N., Dedera D. Inhibition of HIV and SIV infectivity by blockade of alpha-glucosidase activity. Virology. 1991 Mar;181(1):180–192. doi: 10.1016/0042-6822(91)90483-r. [DOI] [PubMed] [Google Scholar]
- Rausch D. M., Lifson J. D., Padgett M. P., Chandrasekhar B., Lendvay J., Hwang K. M., Eiden L. E. CD4(81-92)-based peptide derivatives. Structural requirements for blockade of HIV infection, blockade of HIV-induced syncytium formation, and virostatic activity in vitro. Biochem Pharmacol. 1992 Apr 15;43(8):1785–1796. doi: 10.1016/0006-2952(92)90711-q. [DOI] [PubMed] [Google Scholar]
- Rice W. G., Schaeffer C. A., Harten B., Villinger F., South T. L., Summers M. F., Henderson L. E., Bess J. W., Jr, Arthur L. O., McDougal J. S. Inhibition of HIV-1 infectivity by zinc-ejecting aromatic C-nitroso compounds. Nature. 1993 Feb 4;361(6411):473–475. doi: 10.1038/361473a0. [DOI] [PubMed] [Google Scholar]
- Rich D. H., Sun C. Q., Vara Prasad J. V., Pathiasseril A., Toth M. V., Marshall G. R., Clare M., Mueller R. A., Houseman K. Effect of hydroxyl group configuration in hydroxyethylamine dipeptide isosteres on HIV protease inhibition. Evidence for multiple binding modes. J Med Chem. 1991 Mar;34(3):1222–1225. doi: 10.1021/jm00107a049. [DOI] [PubMed] [Google Scholar]
- Richman D. D., Meng T. C., Spector S. A., Fischl M. A., Resnick L., Lai S. Resistance to AZT and ddC during long-term combination therapy in patients with advanced infection with human immunodeficiency virus. J Acquir Immune Defic Syndr. 1994 Feb;7(2):135–138. [PubMed] [Google Scholar]
- Richman D., Rosenthal A. S., Skoog M., Eckner R. J., Chou T. C., Sabo J. P., Merluzzi V. J. BI-RG-587 is active against zidovudine-resistant human immunodeficiency virus type 1 and synergistic with zidovudine. Antimicrob Agents Chemother. 1991 Feb;35(2):305–308. doi: 10.1128/aac.35.2.305. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Richman D., Shih C. K., Lowy I., Rose J., Prodanovich P., Goff S., Griffin J. Human immunodeficiency virus type 1 mutants resistant to nonnucleoside inhibitors of reverse transcriptase arise in tissue culture. Proc Natl Acad Sci U S A. 1991 Dec 15;88(24):11241–11245. doi: 10.1073/pnas.88.24.11241. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Rittner K., Sczakiel G. Identification and analysis of antisense RNA target regions of the human immunodeficiency virus type 1. Nucleic Acids Res. 1991 Apr 11;19(7):1421–1426. doi: 10.1093/nar/19.7.1421. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Roberts N. A., Martin J. A., Kinchington D., Broadhurst A. V., Craig J. C., Duncan I. B., Galpin S. A., Handa B. K., Kay J., Kröhn A. Rational design of peptide-based HIV proteinase inhibitors. Science. 1990 Apr 20;248(4953):358–361. doi: 10.1126/science.2183354. [DOI] [PubMed] [Google Scholar]
- Romero D. L., Busso M., Tan C. K., Reusser F., Palmer J. R., Poppe S. M., Aristoff P. A., Downey K. M., So A. G., Resnick L. Nonnucleoside reverse transcriptase inhibitors that potently and specifically block human immunodeficiency virus type 1 replication. Proc Natl Acad Sci U S A. 1991 Oct 1;88(19):8806–8810. doi: 10.1073/pnas.88.19.8806. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Romero D. L., Morge R. A., Genin M. J., Biles C., Busso M., Resnick L., Althaus I. W., Reusser F., Thomas R. C., Tarpley W. G. Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piperazine monomethanesulfonate (U-90152S), a second-generation clinical candidate. J Med Chem. 1993 May 14;36(10):1505–1508. doi: 10.1021/jm00062a027. [DOI] [PubMed] [Google Scholar]
- Rosenwirth B., Billich A., Datema R., Donatsch P., Hammerschmid F., Harrison R., Hiestand P., Jaksche H., Mayer P., Peichl P. Inhibition of human immunodeficiency virus type 1 replication by SDZ NIM 811, a nonimmunosuppressive cyclosporine analog. Antimicrob Agents Chemother. 1994 Aug;38(8):1763–1772. doi: 10.1128/aac.38.8.1763. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Rossi J. J., Cantin E. M., Sarver N., Chang P. F. The potential use of catalytic RNAs in therapy of HIV infection and other diseases. Pharmacol Ther. 1991;50(2):245–254. doi: 10.1016/0163-7258(91)90016-f. [DOI] [PubMed] [Google Scholar]
- Rossi J. J., Elkins D., Zaia J. A., Sullivan S. Ribozymes as anti-HIV-1 therapeutic agents: principles, applications, and problems. AIDS Res Hum Retroviruses. 1992 Feb;8(2):183–189. doi: 10.1089/aid.1992.8.183. [DOI] [PubMed] [Google Scholar]
- Ruprecht R. M., Bernard L. D., Bronson R., Gama Sosa M. A., Mullaney S. Castanospermine vs. its 6-O-butanoyl analog: a comparison of toxicity and antiviral activity in vitro and in vivo. J Acquir Immune Defic Syndr. 1991;4(1):48–55. [PubMed] [Google Scholar]
- Ruprecht R. M., Mullaney S., Andersen J., Bronson R. In vivo analysis of castanospermine, a candidate antiretroviral agent. J Acquir Immune Defic Syndr. 1989;2(2):149–157. [PubMed] [Google Scholar]
- Ruprecht R. M., Rossoni L. D., Haseltine W. A., Broder S. Suppression of retroviral propagation and disease by suramin in murine systems. Proc Natl Acad Sci U S A. 1985 Nov;82(22):7733–7737. doi: 10.1073/pnas.82.22.7733. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Saag M. S., Emini E. A., Laskin O. L., Douglas J., Lapidus W. I., Schleif W. A., Whitley R. J., Hildebrand C., Byrnes V. W., Kappes J. C. A short-term clinical evaluation of L-697,661, a non-nucleoside inhibitor of HIV-1 reverse transcriptase. L-697,661 Working Group. N Engl J Med. 1993 Oct 7;329(15):1065–1072. doi: 10.1056/NEJM199310073291502. [DOI] [PubMed] [Google Scholar]
- Sardana V. V., Emini E. A., Gotlib L., Graham D. J., Lineberger D. W., Long W. J., Schlabach A. J., Wolfgang J. A., Condra J. H. Functional analysis of HIV-1 reverse transcriptase amino acids involved in resistance to multiple nonnucleoside inhibitors. J Biol Chem. 1992 Sep 5;267(25):17526–17530. [PubMed] [Google Scholar]
- Sarin P. S., Agrawal S., Civeira M. P., Goodchild J., Ikeuchi T., Zamecnik P. C. Inhibition of acquired immunodeficiency syndrome virus by oligodeoxynucleoside methylphosphonates. Proc Natl Acad Sci U S A. 1988 Oct;85(20):7448–7451. doi: 10.1073/pnas.85.20.7448. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Sarin P. S., Sun D., Thornton A., Müller W. E. Inhibition of replication of the etiologic agent of acquired immune deficiency syndrome (human T-lymphotropic retrovirus/lymphadenopathy-associated virus) by avarol and avarone. J Natl Cancer Inst. 1987 Apr;78(4):663–666. [PubMed] [Google Scholar]
- Sarver N., Cantin E. M., Chang P. S., Zaia J. A., Ladne P. A., Stephens D. A., Rossi J. J. Ribozymes as potential anti-HIV-1 therapeutic agents. Science. 1990 Mar 9;247(4947):1222–1225. doi: 10.1126/science.2107573. [DOI] [PubMed] [Google Scholar]
- Schinazi R. F., Boudinot F. D., Ibrahim S. S., Manning C., McClure H. M., Liotta D. C. Pharmacokinetics and metabolism of racemic 2',3'-dideoxy-5-fluoro-3'-thiacytidine in rhesus monkeys. Antimicrob Agents Chemother. 1992 Nov;36(11):2432–2438. doi: 10.1128/aac.36.11.2432. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Schinazi R. F., Chu C. K., Peck A., McMillan A., Mathis R., Cannon D., Jeong L. S., Beach J. W., Choi W. B., Yeola S. Activities of the four optical isomers of 2',3'-dideoxy-3'-thiacytidine (BCH-189) against human immunodeficiency virus type 1 in human lymphocytes. Antimicrob Agents Chemother. 1992 Mar;36(3):672–676. doi: 10.1128/aac.36.3.672. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Schinazi R. F., Lloyd R. M., Jr, Nguyen M. H., Cannon D. L., McMillan A., Ilksoy N., Chu C. K., Liotta D. C., Bazmi H. Z., Mellors J. W. Characterization of human immunodeficiency viruses resistant to oxathiolane-cytosine nucleosides. Antimicrob Agents Chemother. 1993 Apr;37(4):875–881. doi: 10.1128/aac.37.4.875. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Schinazi R. F., Lloyd R. M., Jr, Ramanathan C. S., Taylor E. W. Antiviral drug resistance mutations in human immunodeficiency virus type 1 reverse transcriptase occur in specific RNA structural regions. Antimicrob Agents Chemother. 1994 Feb;38(2):268–274. doi: 10.1128/aac.38.2.268. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Schinazi R. F., McMillan A., Cannon D., Mathis R., Lloyd R. M., Peck A., Sommadossi J. P., St Clair M., Wilson J., Furman P. A. Selective inhibition of human immunodeficiency viruses by racemates and enantiomers of cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine. Antimicrob Agents Chemother. 1992 Nov;36(11):2423–2431. doi: 10.1128/aac.36.11.2423. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Schinazi R. F., Mead J. R., Feorino P. M. Insights into HIV chemotherapy. AIDS Res Hum Retroviruses. 1992 Jun;8(6):963–990. doi: 10.1089/aid.1992.8.963. [DOI] [PubMed] [Google Scholar]
- Schinazi R. F., Sijbesma R., Srdanov G., Hill C. L., Wudl F. Synthesis and virucidal activity of a water-soluble, configurationally stable, derivatized C60 fullerene. Antimicrob Agents Chemother. 1993 Aug;37(8):1707–1710. doi: 10.1128/aac.37.8.1707. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Schols D., Baba M., Pauwels R., De Clercq E. Flow cytometric method to demonstrate whether anti-HIV-1 agents inhibit virion binding to T4+ cells. J Acquir Immune Defic Syndr. 1989;2(1):10–15. [PubMed] [Google Scholar]
- Schols D., Baba M., Pauwels R., Desmyter J., De Clercq E. Specific interaction of aurintricarboxylic acid with the human immunodeficiency virus/CD4 cell receptor. Proc Natl Acad Sci U S A. 1989 May;86(9):3322–3326. doi: 10.1073/pnas.86.9.3322. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Schols D., Wutzler P., Klöcking R., Helbig B., De Clercq E. Selective inhibitory activity of polyhydroxycarboxylates derived from phenolic compounds against human immunodeficiency virus replication. J Acquir Immune Defic Syndr. 1991;4(7):677–685. [PubMed] [Google Scholar]
- Schäfer W., Friebe W. G., Leinert H., Mertens A., Poll T., von der Saal W., Zilch H., Nuber B., Ziegler M. L. Non-nucleoside inhibitors of HIV-1 reverse transcriptase: molecular modeling and X-ray structure investigations. J Med Chem. 1993 Mar 19;36(6):726–732. doi: 10.1021/jm00058a009. [DOI] [PubMed] [Google Scholar]
- Shapira-Nahor O., Golding H., Vujcic L. K., Resto-Ruiz S., Fields R. L., Robey F. A. CD4-derived synthetic peptide blocks the binding of HIV-1 GP120 to CD4-bearing cells and prevents HIV-1 infection. Cell Immunol. 1990 Jun;128(1):101–117. doi: 10.1016/0008-8749(90)90010-o. [DOI] [PubMed] [Google Scholar]
- Shibuya H., Irie K., Ninomiya-Tsuji J., Goebl M., Taniguchi T., Matsumoto K. New human gene encoding a positive modulator of HIV Tat-mediated transactivation. Nature. 1992 Jun 25;357(6380):700–702. doi: 10.1038/357700a0. [DOI] [PubMed] [Google Scholar]
- Shih C. K., Rose J. M., Hansen G. L., Wu J. C., Bacolla A., Griffin J. A. Chimeric human immunodeficiency virus type 1/type 2 reverse transcriptases display reversed sensitivity to nonnucleoside analog inhibitors. Proc Natl Acad Sci U S A. 1991 Nov 1;88(21):9878–9882. doi: 10.1073/pnas.88.21.9878. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Shimizu H., Tsuchie H., Yoshida K., Morikawa S., Tsuruoka T., Yamamoto H., Ushijima H., Kitamura T. Inhibitory effect of novel 1-deoxynojirimycin derivatives on HIV-1 replication. AIDS. 1990 Oct;4(10):975–979. doi: 10.1097/00002030-199010000-00005. [DOI] [PubMed] [Google Scholar]
- Shirazi Y., Pitha P. M. Interferon alpha-mediated inhibition of human immunodeficiency virus type 1 provirus synthesis in T-cells. Virology. 1993 Mar;193(1):303–312. doi: 10.1006/viro.1993.1126. [DOI] [PubMed] [Google Scholar]
- Sioud M., Drlica K. Prevention of human immunodeficiency virus type 1 integrase expression in Escherichia coli by a ribozyme. Proc Natl Acad Sci U S A. 1991 Aug 15;88(16):7303–7307. doi: 10.1073/pnas.88.16.7303. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Smith M. S., Brian E. L., De Clercq E., Pagano J. S. Susceptibility of human immunodeficiency virus type 1 replication in vitro to acyclic adenosine analogs and synergy of the analogs with 3'-azido-3'-deoxythymidine. Antimicrob Agents Chemother. 1989 Sep;33(9):1482–1486. doi: 10.1128/aac.33.9.1482. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Smith M. S., Brian E. L., Pagano J. S. Resumption of virus production after human immunodeficiency virus infection of T lymphocytes in the presence of azidothymidine. J Virol. 1987 Dec;61(12):3769–3773. doi: 10.1128/jvi.61.12.3769-3773.1987. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Smith M. S., Thresher R. J., Pagano J. S. Inhibition of human immunodeficiency virus type 1 morphogenesis in T cells by alpha interferon. Antimicrob Agents Chemother. 1991 Jan;35(1):62–67. doi: 10.1128/aac.35.1.62. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Soudeyns H., Yao X. I., Gao Q., Belleau B., Kraus J. L., Nguyen-Ba N., Spira B., Wainberg M. A. Anti-human immunodeficiency virus type 1 activity and in vitro toxicity of 2'-deoxy-3'-thiacytidine (BCH-189), a novel heterocyclic nucleoside analog. Antimicrob Agents Chemother. 1991 Jul;35(7):1386–1390. doi: 10.1128/aac.35.7.1386. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Spector S. A., Ripley D., Hsia K. Human immunodeficiency virus inhibition is prolonged by 3'-azido-3'-deoxythymidine alternating with 2',3'-dideoxycytidine compared with 3'-azido-3'-deoxythymidine alone. Antimicrob Agents Chemother. 1989 Jun;33(6):920–923. doi: 10.1128/aac.33.6.920. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Srinivas R. V., Robbins B. L., Connelly M. C., Gong Y. F., Bischofberger N., Fridland A. Metabolism and in vitro antiretroviral activities of bis(pivaloyloxymethyl) prodrugs of acyclic nucleoside phosphonates. Antimicrob Agents Chemother. 1993 Oct;37(10):2247–2250. doi: 10.1128/aac.37.10.2247. [DOI] [PMC free article] [PubMed] [Google Scholar]
- St Clair M. H., Martin J. L., Tudor-Williams G., Bach M. C., Vavro C. L., King D. M., Kellam P., Kemp S. D., Larder B. A. Resistance to ddI and sensitivity to AZT induced by a mutation in HIV-1 reverse transcriptase. Science. 1991 Sep 27;253(5027):1557–1559. doi: 10.1126/science.1716788. [DOI] [PubMed] [Google Scholar]
- St Clair M. H., Richards C. A., Spector T., Weinhold K. J., Miller W. H., Langlois A. J., Furman P. A. 3'-Azido-3'-deoxythymidine triphosphate as an inhibitor and substrate of purified human immunodeficiency virus reverse transcriptase. Antimicrob Agents Chemother. 1987 Dec;31(12):1972–1977. doi: 10.1128/aac.31.12.1972. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Starrett J. E., Jr, Tortolani D. R., Hitchcock M. J., Martin J. C., Mansuri M. M. Synthesis and in vitro evaluation of a phosphonate prodrug: bis(pivaloyloxymethyl) 9-(2-phosphonylmethoxyethyl)adenine. Antiviral Res. 1992 Sep;19(3):267–273. doi: 10.1016/0166-3542(92)90084-i. [DOI] [PubMed] [Google Scholar]
- Stevenson N. R., Lenard J. Antiretroviral activities of hypericin and rose bengal: photodynamic effects on Friend leukemia virus infection of mice. Antiviral Res. 1993 Jun;21(2):119–127. doi: 10.1016/0166-3542(93)90048-n. [DOI] [PubMed] [Google Scholar]
- Sullenger B. A., Cech T. R. Tethering ribozymes to a retroviral packaging signal for destruction of viral RNA. Science. 1993 Dec 3;262(5139):1566–1569. doi: 10.1126/science.8248806. [DOI] [PubMed] [Google Scholar]
- Takahashi I., Nakanishi S., Kobayashi E., Nakano H., Suzuki K., Tamaoki T. Hypericin and pseudohypericin specifically inhibit protein kinase C: possible relation to their antiretroviral activity. Biochem Biophys Res Commun. 1989 Dec 29;165(3):1207–1212. doi: 10.1016/0006-291x(89)92730-7. [DOI] [PubMed] [Google Scholar]
- Take Y., Tokutake Y., Inouye Y., Yoshida T., Yamamoto A., Yamase T., Nakamura S. Inhibition of proliferation of human immunodeficiency virus type 1 by novel heteropolyoxotungstates in vitro. Antiviral Res. 1991 Feb;15(2):113–124. doi: 10.1016/0166-3542(91)90029-q. [DOI] [PubMed] [Google Scholar]
- Tamura Y., Lai P. K., Bradley W. G., Konno K., Tanaka A., Nonoyama M. A soluble factor induced by an extract from Pinus parviflora Sieb et Zucc can inhibit the replication of human immunodeficiency virus in vitro. Proc Natl Acad Sci U S A. 1991 Mar 15;88(6):2249–2253. doi: 10.1073/pnas.88.6.2249. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Tan C. K., Civil R., Mian A. M., So A. G., Downey K. M. Inhibition of the RNase H activity of HIV reverse transcriptase by azidothymidylate. Biochemistry. 1991 May 21;30(20):4831–4835. doi: 10.1021/bi00234a001. [DOI] [PubMed] [Google Scholar]
- Tan G. T., Kinghorn A. D., Hughes S. H., Pezzuto J. M. Psychotrine and its O-methyl ether are selective inhibitors of human immunodeficiency virus-1 reverse transcriptase. J Biol Chem. 1991 Dec 15;266(35):23529–23536. [PubMed] [Google Scholar]
- Tanabe-Tochikura A., Tochikura T. S., Yoshida O., Oki T., Yamamoto N. Pradimicin A inhibition of human immunodeficiency virus: attenuation by mannan. Virology. 1990 Jun;176(2):467–473. doi: 10.1016/0042-6822(90)90016-k. [DOI] [PubMed] [Google Scholar]
- Tang J. Y., Temsamani J., Agrawal S. Self-stabilized antisense oligodeoxynucleotide phosphorothioates: properties and anti-HIV activity. Nucleic Acids Res. 1993 Jun 11;21(11):2729–2735. doi: 10.1093/nar/21.11.2729. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Tang J., Colacino J. M., Larsen S. H., Spitzer W. Virucidal activity of hypericin against enveloped and non-enveloped DNA and RNA viruses. Antiviral Res. 1990 Jun;13(6):313–325. doi: 10.1016/0166-3542(90)90015-y. [DOI] [PubMed] [Google Scholar]
- Tantillo C., Ding J., Jacobo-Molina A., Nanni R. G., Boyer P. L., Hughes S. H., Pauwels R., Andries K., Janssen P. A., Arnold E. Locations of anti-AIDS drug binding sites and resistance mutations in the three-dimensional structure of HIV-1 reverse transcriptase. Implications for mechanisms of drug inhibition and resistance. J Mol Biol. 1994 Oct 28;243(3):369–387. doi: 10.1006/jmbi.1994.1665. [DOI] [PubMed] [Google Scholar]
- Tashiro A., Shoji S., Kubota Y. Antimyristoylation of the gag proteins in the human immunodeficiency virus-infected cells with N-myristoyl glycinal diethylacetal resulted in inhibition of virus production. Biochem Biophys Res Commun. 1989 Dec 29;165(3):1145–1154. doi: 10.1016/0006-291x(89)92722-8. [DOI] [PubMed] [Google Scholar]
- Thaisrivongs S., Turner S. R., Strohbach J. W., TenBrink R. E., Tarpley W. G., McQuade T. J., Heinrikson R. L., Tomasselli A. G., Hui J. O., Howe W. J. Inhibitors of the protease from human immunodeficiency virus: synthesis, enzyme inhibition, and antiviral activity of a series of compounds containing the dihydroxyethylene transition-state isostere. J Med Chem. 1993 Apr 16;36(8):941–952. doi: 10.1021/jm00060a001. [DOI] [PubMed] [Google Scholar]
- Thormar H., Balzarini J., Holy A., Jindrich J., Rosenberg I., Debyser Z., Desmyter J., De Clercq E. Inhibition of visna virus replication by 2',3'-dideoxynucleosides and acyclic nucleoside phosphonate analogs. Antimicrob Agents Chemother. 1993 Dec;37(12):2540–2544. doi: 10.1128/aac.37.12.2540. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Tisdale M., Kemp S. D., Parry N. R., Larder B. A. Rapid in vitro selection of human immunodeficiency virus type 1 resistant to 3'-thiacytidine inhibitors due to a mutation in the YMDD region of reverse transcriptase. Proc Natl Acad Sci U S A. 1993 Jun 15;90(12):5653–5656. doi: 10.1073/pnas.90.12.5653. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Tochikura T. S., Nakashima H., Yamamoto N. Antiviral agents with activity against human retroviruses. J Acquir Immune Defic Syndr. 1989;2(5):441–447. [PubMed] [Google Scholar]
- Tomasselli A. G., Hui J. O., Sawyer T. K., Staples D. J., Bannow C., Reardon I. M., Howe W. J., DeCamp D. L., Craik C. S., Heinrikson R. L. Specificity and inhibition of proteases from human immunodeficiency viruses 1 and 2. J Biol Chem. 1990 Aug 25;265(24):14675–14683. [PubMed] [Google Scholar]
- Tramontano E., Cheng Y. C. HIV-1 reverse transcriptase inhibition by a dipyridodiazepinone derivative: BI-RG-587. Biochem Pharmacol. 1992 Mar 17;43(6):1371–1376. doi: 10.1016/0006-2952(92)90515-k. [DOI] [PubMed] [Google Scholar]
- Tsai C. C., Follis K. E., Sabo A., Grant R. F., Bartz C., Nolte R. E., Benveniste R. E., Bischofberger N. Preexposure prophylaxis with 9-(2-phosphonylmethoxyethyl)adenine against simian immunodeficiency virus infection in macaques. J Infect Dis. 1994 Feb;169(2):260–266. doi: 10.1093/infdis/169.2.260. [DOI] [PubMed] [Google Scholar]
- Tsuchihashi Z., Khosla M., Herschlag D. Protein enhancement of hammerhead ribozyme catalysis. Science. 1993 Oct 1;262(5130):99–102. doi: 10.1126/science.7692597. [DOI] [PubMed] [Google Scholar]
- Tucker T. J., Lyle T. A., Wiscount C. M., Britcher S. F., Young S. D., Sanders W. M., Lumma W. C., Goldman M. E., O'Brien J. A., Ball R. G. Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. J Med Chem. 1994 Jul 22;37(15):2437–2444. doi: 10.1021/jm00041a023. [DOI] [PubMed] [Google Scholar]
- Tuerk C., MacDougal S., Gold L. RNA pseudoknots that inhibit human immunodeficiency virus type 1 reverse transcriptase. Proc Natl Acad Sci U S A. 1992 Aug 1;89(15):6988–6992. doi: 10.1073/pnas.89.15.6988. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Tung F. Y., Daniel M. D. Targeted inhibition of immunodeficiency virus replication in lymphocytes through retroviral mediated gene transfer. Arch Virol. 1993;133(3-4):407–421. doi: 10.1007/BF01313779. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Uryu T., Ikushima N., Katsuraya K., Shoji T., Takahashi N., Yoshida T., Kanno K., Murakami T., Nakashima H., Yamamoto N. Sulfated alkyl oligosaccharides with potent inhibitory effects on human immunodeficiency virus infection. Biochem Pharmacol. 1992 Jun 9;43(11):2385–2392. doi: 10.1016/0006-2952(92)90317-c. [DOI] [PubMed] [Google Scholar]
- Vacca J. P., Guare J. P., deSolms S. J., Sanders W. M., Giuliani E. A., Young S. D., Darke P. L., Zugay J., Sigal I. S., Schleif W. A. L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor. J Med Chem. 1991 Mar;34(3):1225–1228. doi: 10.1021/jm00107a050. [DOI] [PubMed] [Google Scholar]
- Van Aerschot A., Herdewijn P., Balzarini J., Pauwels R., De Clercq E. 3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues. J Med Chem. 1989 Aug;32(8):1743–1749. doi: 10.1021/jm00128a013. [DOI] [PubMed] [Google Scholar]
- Vandamme A. M., Debyser Z., Pauwels R., De Vreese K., Goubau P., Youle M., Gazzard B., Stoffels P. A., Cauwenbergh G. F., Anne J. Characterization of HIV-1 strains isolated from patients treated with TIBO R82913. AIDS Res Hum Retroviruses. 1994 Jan;10(1):39–46. doi: 10.1089/aid.1994.10.39. [DOI] [PubMed] [Google Scholar]
- Vasudevachari M. B., Battista C., Lane H. C., Psallidopoulos M. C., Zhao B., Cook J., Palmer J. R., Romero D. L., Tarpley W. G., Salzman N. P. Prevention of the spread of HIV-1 infection with nonnucleoside reverse transcriptase inhibitors. Virology. 1992 Sep;190(1):269–277. doi: 10.1016/0042-6822(92)91213-e. [DOI] [PubMed] [Google Scholar]
- Vink C., van Gent D. C., Elgersma Y., Plasterk R. H. Human immunodeficiency virus integrase protein requires a subterminal position of its viral DNA recognition sequence for efficient cleavage. J Virol. 1991 Sep;65(9):4636–4644. doi: 10.1128/jvi.65.9.4636-4644.1991. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Vogt M. W., Durno A. G., Chou T. C., Coleman L. A., Paradis T. J., Schooley R. T., Kaplan J. C., Hirsch M. S. Synergistic interaction of 2',3'-dideoxycytidine and recombinant interferon-alpha-A on replication of human immunodeficiency virus type 1. J Infect Dis. 1988 Aug;158(2):378–385. doi: 10.1093/infdis/158.2.378. [DOI] [PubMed] [Google Scholar]
- Vogt M. W., Hartshorn K. L., Furman P. A., Chou T. C., Fyfe J. A., Coleman L. A., Crumpacker C., Schooley R. T., Hirsch M. S. Ribavirin antagonizes the effect of azidothymidine on HIV replication. Science. 1987 Mar 13;235(4794):1376–1379. doi: 10.1126/science.2435003. [DOI] [PubMed] [Google Scholar]
- Walker B. D., Kowalski M., Goh W. C., Kozarsky K., Krieger M., Rosen C., Rohrschneider L., Haseltine W. A., Sodroski J. Inhibition of human immunodeficiency virus syncytium formation and virus replication by castanospermine. Proc Natl Acad Sci U S A. 1987 Nov;84(22):8120–8124. doi: 10.1073/pnas.84.22.8120. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Ward R. H., Capon D. J., Jett C. M., Murthy K. K., Mordenti J., Lucas C., Frie S. W., Prince A. M., Green J. D., Eichberg J. W. Prevention of HIV-1 IIIB infection in chimpanzees by CD4 immunoadhesin. Nature. 1991 Aug 1;352(6334):434–436. doi: 10.1038/352434a0. [DOI] [PubMed] [Google Scholar]
- Weaver J. L., Gergely P., Pine P. S., Patzer E., Aszalos A. Polyionic compounds selectively alter availability of CD4 receptors for HIV coat protein rgp120. AIDS Res Hum Retroviruses. 1990 Sep;6(9):1125–1130. doi: 10.1089/aid.1990.6.1125. [DOI] [PubMed] [Google Scholar]
- Weaver J. L., Pine P. S., Dutschman G., Cheng Y. C., Lee K. H., Aszalos A. Prevention of binding of rgp120 by anti-HIV active tannins. Biochem Pharmacol. 1992 Jun 9;43(11):2479–2480. doi: 10.1016/0006-2952(92)90328-g. [DOI] [PubMed] [Google Scholar]
- Weeks M. S., Hill C. L., Schinazi R. F. Synthesis, characterization, and anti-human immunodeficiency virus activity of water-soluble salts of polyoxotungstate anions with covalently attached organic groups. J Med Chem. 1992 Apr 3;35(7):1216–1221. doi: 10.1021/jm00085a008. [DOI] [PubMed] [Google Scholar]
- Weerasinghe M., Liem S. E., Asad S., Read S. E., Joshi S. Resistance to human immunodeficiency virus type 1 (HIV-1) infection in human CD4+ lymphocyte-derived cell lines conferred by using retroviral vectors expressing an HIV-1 RNA-specific ribozyme. J Virol. 1991 Oct;65(10):5531–5534. doi: 10.1128/jvi.65.10.5531-5534.1991. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Weiler B. E., Schröder H. C., Stefanovich V., Stewart D., Forrest J. M., Allen L. B., Bowden B. J., Kreuter M. H., Voth R., Müller W. E. Sulphoevernan, a polyanionic polysaccharide, and the narcissus lectin potently inhibit human immunodeficiency virus infection by binding to viral envelope protein. J Gen Virol. 1990 Sep;71(Pt 9):1957–1963. doi: 10.1099/0022-1317-71-9-1957. [DOI] [PubMed] [Google Scholar]
- White E. L., Buckheit R. W., Jr, Ross L. J., Germany J. M., Andries K., Pauwels R., Janssen P. A., Shannon W. M., Chirigos M. A. A TIBO derivative, R82913, is a potent inhibitor of HIV-1 reverse transcriptase with heteropolymer templates. Antiviral Res. 1991 Oct;16(3):257–266. doi: 10.1016/0166-3542(91)90005-c. [DOI] [PubMed] [Google Scholar]
- Whittington R., Brogden R. N. Zalcitabine. A review of its pharmacology and clinical potential in acquired immunodeficiency syndrome (AIDS). Drugs. 1992 Oct;44(4):656–683. doi: 10.2165/00003495-199244040-00009. [DOI] [PubMed] [Google Scholar]
- Williams T. M., Ciccarone T. M., MacTough S. C., Rooney C. S., Balani S. K., Condra J. H., Emini E. A., Goldman M. E., Greenlee W. J., Kauffman L. R. 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. J Med Chem. 1993 Apr 30;36(9):1291–1294. doi: 10.1021/jm00061a022. [DOI] [PubMed] [Google Scholar]
- Wilson J. E., Martin J. L., Borroto-Esoda K., Hopkins S., Painter G., Liotta D. C., Furman P. A. The 5'-triphosphates of the (-) and (+) enantiomers of cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolane-5-yl]cytosine equally inhibit human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1993 Aug;37(8):1720–1722. doi: 10.1128/aac.37.8.1720. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Winkler D. A., Holan G. Design of potential anti-HIV agents. 1. Mannosidase inhibitors. J Med Chem. 1989 Sep;32(9):2084–2089. doi: 10.1021/jm00129a011. [DOI] [PubMed] [Google Scholar]
- Witvrouw M., Pauwels R., Vandamme A. M., Schols D., Reymen D., Yamamoto N., Desmyter J., De Clercq E. Cell type-specific anti-human immunodeficiency virus type 1 activity of the transactivation inhibitor Ro5-3335. Antimicrob Agents Chemother. 1992 Dec;36(12):2628–2633. doi: 10.1128/aac.36.12.2628. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Wlodawer A., Erickson J. W. Structure-based inhibitors of HIV-1 protease. Annu Rev Biochem. 1993;62:543–585. doi: 10.1146/annurev.bi.62.070193.002551. [DOI] [PubMed] [Google Scholar]
- Wu J. C., Warren T. C., Adams J., Proudfoot J., Skiles J., Raghavan P., Perry C., Potocki I., Farina P. R., Grob P. M. A novel dipyridodiazepinone inhibitor of HIV-1 reverse transcriptase acts through a nonsubstrate binding site. Biochemistry. 1991 Feb 26;30(8):2022–2026. doi: 10.1021/bi00222a003. [DOI] [PubMed] [Google Scholar]
- Yamamoto N., Schols D., De Clercq E., Debyser Z., Pauwels R., Balzarini J., Nakashima H., Baba M., Hosoya M., Snoeck R. Mechanism of anti-human immunodeficiency virus action of polyoxometalates, a class of broad-spectrum antiviral agents. Mol Pharmacol. 1992 Dec;42(6):1109–1117. [PubMed] [Google Scholar]
- Yao X. J., Wainberg M. A., Parniak M. A. Mechanism of inhibition of HIV-1 infection in vitro by purified extract of Prunella vulgaris. Virology. 1992 Mar;187(1):56–62. doi: 10.1016/0042-6822(92)90294-y. [DOI] [PubMed] [Google Scholar]
- Yao X. J., Wainberg M. A., Richard M., Pollak M. The ability of suramin to block CD4-gp120 binding is reversed in the presence of albumin. Antimicrob Agents Chemother. 1991 Dec;35(12):2636–2638. doi: 10.1128/aac.35.12.2636. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Yarchoan R., Mitsuya H., Broder S. Challenges in the therapy of HIV infection. Trends Pharmacol Sci. 1993 May;14(5):196–202. doi: 10.1016/0165-6147(93)90208-2. [DOI] [PubMed] [Google Scholar]
- Yeh P., Landais D., Lemaître M., Maury I., Crenne J. Y., Becquart J., Murry-Brelier A., Boucher F., Montay G., Fleer R. Design of yeast-secreted albumin derivatives for human therapy: biological and antiviral properties of a serum albumin-CD4 genetic conjugate. Proc Natl Acad Sci U S A. 1992 Mar 1;89(5):1904–1908. doi: 10.1073/pnas.89.5.1904. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Yokota T., Konno K., Chonan E., Mochizuki S., Kojima K., Shigeta S., de Clercq E. Comparative activities of several nucleoside analogs against duck hepatitis B virus in vitro. Antimicrob Agents Chemother. 1990 Jul;34(7):1326–1330. doi: 10.1128/aac.34.7.1326. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Yokota T., Mochizuki S., Konno K., Mori S., Shigeta S., De Clercq E. Inhibitory effects of selected antiviral compounds on human hepatitis B virus DNA synthesis. Antimicrob Agents Chemother. 1991 Feb;35(2):394–397. doi: 10.1128/aac.35.2.394. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Yu M., Ojwang J., Yamada O., Hampel A., Rapapport J., Looney D., Wong-Staal F. A hairpin ribozyme inhibits expression of diverse strains of human immunodeficiency virus type 1. Proc Natl Acad Sci U S A. 1993 Jul 1;90(13):6340–6344. doi: 10.1073/pnas.90.13.6340. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Yuasa S., Sadakata Y., Takashima H., Sekiya K., Inouye N., Ubasawa M., Baba M. Selective and synergistic inhibition of human immunodeficiency virus type 1 reverse transcriptase by a non-nucleoside inhibitor, MKC-442. Mol Pharmacol. 1993 Oct;44(4):895–900. [PubMed] [Google Scholar]
- Yusa K., Oh-hara T., Tsukahara S., Baba K., Taniguchi M., Kozawa M., Takeuchi S., Hara H., Tsuruo T. Inhibition of human immunodeficiency virus type 1 (HIV-1) replication by daphnodorins. Antiviral Res. 1994 Sep;25(1):57–66. doi: 10.1016/0166-3542(94)90093-0. [DOI] [PubMed] [Google Scholar]
- Zamecnik P. C., Goodchild J., Taguchi Y., Sarin P. S. Inhibition of replication and expression of human T-cell lymphotropic virus type III in cultured cells by exogenous synthetic oligonucleotides complementary to viral RNA. Proc Natl Acad Sci U S A. 1986 Jun;83(12):4143–4146. doi: 10.1073/pnas.83.12.4143. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Zarling J. M., Moran P. A., Haffar O., Sias J., Richman D. D., Spina C. A., Myers D. E., Kuebelbeck V., Ledbetter J. A., Uckun F. M. Inhibition of HIV replication by pokeweed antiviral protein targeted to CD4+ cells by monoclonal antibodies. Nature. 1990 Sep 6;347(6288):92–95. doi: 10.1038/347092a0. [DOI] [PubMed] [Google Scholar]
- Zhang D., Caliendo A. M., Eron J. J., DeVore K. M., Kaplan J. C., Hirsch M. S., D'Aquila R. T. Resistance to 2',3'-dideoxycytidine conferred by a mutation in codon 65 of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1994 Feb;38(2):282–287. doi: 10.1128/aac.38.2.282. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Zhang H., Vrang L., Bäckbro K., Unge T., Noréen R., Oberg B. Enzymatic properties and sensitivity to inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase with Glu-138-->Arg and Tyr-188-->His mutations. Antiviral Res. 1994 May;24(1):43–57. doi: 10.1016/0166-3542(94)90051-5. [DOI] [PubMed] [Google Scholar]
- de Vreese K., Debyser Z., Vandamme A. M., Pauwels R., Desmyter J., de Clercq E., Anné J. Resistance of human immunodeficiency virus type 1 reverse transcriptase to TIBO derivatives induced by site-directed mutagenesis. Virology. 1992 Jun;188(2):900–904. doi: 10.1016/0042-6822(92)90550-9. [DOI] [PubMed] [Google Scholar]
- de Witte P., Agostinis P., Van Lint J., Merlevede W., Vandenheede J. R. Inhibition of epidermal growth factor receptor tyrosine kinase activity by hypericin. Biochem Pharmacol. 1993 Dec 3;46(11):1929–1936. doi: 10.1016/0006-2952(93)90633-8. [DOI] [PubMed] [Google Scholar]
- deSolms S. J., Giuliani E. A., Guare J. P., Vacca J. P., Sanders W. M., Graham S. L., Wiggins J. M., Darke P. L., Sigal I. S., Zugay J. A. Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679. J Med Chem. 1991 Sep;34(9):2852–2857. doi: 10.1021/jm00113a025. [DOI] [PubMed] [Google Scholar]