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. 1996 May;40(5):1067–1071. doi: 10.1128/aac.40.5.1067

Synthetic combinatorial libraries: novel discovery strategy for identification of antimicrobial agents.

S E Blondelle 1, E Pérez-Payá 1, R A Houghten 1
PMCID: PMC163267  PMID: 8723442

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Selected References

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  1. Bevins C. L., Zasloff M. Peptides from frog skin. Annu Rev Biochem. 1990;59:395–414. doi: 10.1146/annurev.bi.59.070190.002143. [DOI] [PubMed] [Google Scholar]
  2. Blondelle S. E., Houghten R. A. Design of model amphipathic peptides having potent antimicrobial activities. Biochemistry. 1992 Dec 22;31(50):12688–12694. doi: 10.1021/bi00165a020. [DOI] [PubMed] [Google Scholar]
  3. Blondelle S. E., Ostresh J. M., Houghten R. A., Pérez-Payá E. Induced conformational states of amphipathic peptides in aqueous/lipid environments. Biophys J. 1995 Jan;68(1):351–359. doi: 10.1016/S0006-3495(95)80194-3. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Blondelle S. E., Takahashi E., Dinh K. T., Houghten R. A. The antimicrobial activity of hexapeptides derived from synthetic combinatorial libraries. J Appl Bacteriol. 1995 Jan;78(1):39–46. doi: 10.1111/j.1365-2672.1995.tb01671.x. [DOI] [PubMed] [Google Scholar]
  5. Blondelle S. E., Takahashi E., Houghten R. A., Pérez-Payá E. Rapid identification of compounds with enhanced antimicrobial activity by using conformationally defined combinatorial libraries. Biochem J. 1996 Jan 1;313(Pt 1):141–147. doi: 10.1042/bj3130141. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Blondelle S. E., Takahashi E., Weber P. A., Houghten R. A. Identification of antimicrobial peptides by using combinatorial libraries made up of unnatural amino acids. Antimicrob Agents Chemother. 1994 Oct;38(10):2280–2286. doi: 10.1128/aac.38.10.2280. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Boman H. G., Hultmark D. Cell-free immunity in insects. Annu Rev Microbiol. 1987;41:103–126. doi: 10.1146/annurev.mi.41.100187.000535. [DOI] [PubMed] [Google Scholar]
  8. Brumfitt W., Hamilton-Miller J. Methicillin-resistant Staphylococcus aureus. N Engl J Med. 1989 May 4;320(18):1188–1196. doi: 10.1056/NEJM198905043201806. [DOI] [PubMed] [Google Scholar]
  9. Cho C. Y., Moran E. J., Cherry S. R., Stephans J. C., Fodor S. P., Adams C. L., Sundaram A., Jacobs J. W., Schultz P. G. An unnatural biopolymer. Science. 1993 Sep 3;261(5126):1303–1305. doi: 10.1126/science.7689747. [DOI] [PubMed] [Google Scholar]
  10. Davies J. Inactivation of antibiotics and the dissemination of resistance genes. Science. 1994 Apr 15;264(5157):375–382. doi: 10.1126/science.8153624. [DOI] [PubMed] [Google Scholar]
  11. DeWitt S. H., Kiely J. S., Stankovic C. J., Schroeder M. C., Cody D. M., Pavia M. R. "Diversomers": an approach to nonpeptide, nonoligomeric chemical diversity. Proc Natl Acad Sci U S A. 1993 Aug 1;90(15):6909–6913. doi: 10.1073/pnas.90.15.6909. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Fodor S. P., Read J. L., Pirrung M. C., Stryer L., Lu A. T., Solas D. Light-directed, spatially addressable parallel chemical synthesis. Science. 1991 Feb 15;251(4995):767–773. doi: 10.1126/science.1990438. [DOI] [PubMed] [Google Scholar]
  13. Gallop M. A., Barrett R. W., Dower W. J., Fodor S. P., Gordon E. M. Applications of combinatorial technologies to drug discovery. 1. Background and peptide combinatorial libraries. J Med Chem. 1994 Apr 29;37(9):1233–1251. doi: 10.1021/jm00035a001. [DOI] [PubMed] [Google Scholar]
  14. Geysen H. M., Rodda S. J., Mason T. J. A priori delineation of a peptide which mimics a discontinuous antigenic determinant. Mol Immunol. 1986 Jul;23(7):709–715. doi: 10.1016/0161-5890(86)90081-7. [DOI] [PubMed] [Google Scholar]
  15. Gordon E. M., Barrett R. W., Dower W. J., Fodor S. P., Gallop M. A. Applications of combinatorial technologies to drug discovery. 2. Combinatorial organic synthesis, library screening strategies, and future directions. J Med Chem. 1994 May 13;37(10):1385–1401. doi: 10.1021/jm00036a001. [DOI] [PubMed] [Google Scholar]
  16. Houghten R. A., Appel J. R., Blondelle S. E., Cuervo J. H., Dooley C. T., Pinilla C. The use of synthetic peptide combinatorial libraries for the identification of bioactive peptides. Biotechniques. 1992 Sep;13(3):412–421. [PubMed] [Google Scholar]
  17. Houghten R. A., Bray M. K., Degraw S. T., Kirby C. J. Simplified procedure for carrying out simultaneous multiple hydrogen fluoride cleavages of protected peptide resins. Int J Pept Protein Res. 1986 Jun;27(6):673–678. doi: 10.1111/j.1399-3011.1986.tb01064.x. [DOI] [PubMed] [Google Scholar]
  18. Houghten R. A. General method for the rapid solid-phase synthesis of large numbers of peptides: specificity of antigen-antibody interaction at the level of individual amino acids. Proc Natl Acad Sci U S A. 1985 Aug;82(15):5131–5135. doi: 10.1073/pnas.82.15.5131. [DOI] [PMC free article] [PubMed] [Google Scholar]
  19. Houghten R. A., Pinilla C., Blondelle S. E., Appel J. R., Dooley C. T., Cuervo J. H. Generation and use of synthetic peptide combinatorial libraries for basic research and drug discovery. Nature. 1991 Nov 7;354(6348):84–86. doi: 10.1038/354084a0. [DOI] [PubMed] [Google Scholar]
  20. JAWETZ E. Polymyxin, colistin and bacitracin. Pediatr Clin North Am. 1961 Nov;8:1057–1071. doi: 10.1016/s0031-3955(16)31193-2. [DOI] [PubMed] [Google Scholar]
  21. Lam K. S., Salmon S. E., Hersh E. M., Hruby V. J., Kazmierski W. M., Knapp R. J. A new type of synthetic peptide library for identifying ligand-binding activity. Nature. 1991 Nov 7;354(6348):82–84. doi: 10.1038/354082a0. [DOI] [PubMed] [Google Scholar]
  22. Lyon B. R., Skurray R. Antimicrobial resistance of Staphylococcus aureus: genetic basis. Microbiol Rev. 1987 Mar;51(1):88–134. doi: 10.1128/mr.51.1.88-134.1987. [DOI] [PMC free article] [PubMed] [Google Scholar]
  23. Moore K. S., Bevins C. L., Brasseur M. M., Tomassini N., Turner K., Eck H., Zasloff M. Antimicrobial peptides in the stomach of Xenopus laevis. J Biol Chem. 1991 Oct 15;266(29):19851–19857. [PubMed] [Google Scholar]
  24. Moore K. S., Wehrli S., Roder H., Rogers M., Forrest J. N., Jr, McCrimmon D., Zasloff M. Squalamine: an aminosterol antibiotic from the shark. Proc Natl Acad Sci U S A. 1993 Feb 15;90(4):1354–1358. doi: 10.1073/pnas.90.4.1354. [DOI] [PMC free article] [PubMed] [Google Scholar]
  25. Neu H. C. The crisis in antibiotic resistance. Science. 1992 Aug 21;257(5073):1064–1073. doi: 10.1126/science.257.5073.1064. [DOI] [PubMed] [Google Scholar]
  26. Ostresh J. M., Husar G. M., Blondelle S. E., Dörner B., Weber P. A., Houghten R. A. "Libraries from libraries": chemical transformation of combinatorial libraries to extend the range and repertoire of chemical diversity. Proc Natl Acad Sci U S A. 1994 Nov 8;91(23):11138–11142. doi: 10.1073/pnas.91.23.11138. [DOI] [PMC free article] [PubMed] [Google Scholar]
  27. Pinilla C., Appel J., Blondelle S., Dooley C., Dörner B., Eichler J., Ostresh J., Houghten R. A. A review of the utility of soluble peptide combinatorial libraries. Biopolymers. 1995;37(3):221–240. doi: 10.1002/bip.360370306. [DOI] [PubMed] [Google Scholar]
  28. Saberwal G., Nagaraj R. Cell-lytic and antibacterial peptides that act by perturbing the barrier function of membranes: facets of their conformational features, structure-function correlations and membrane-perturbing abilities. Biochim Biophys Acta. 1994 Jun 29;1197(2):109–131. doi: 10.1016/0304-4157(94)90002-7. [DOI] [PubMed] [Google Scholar]
  29. Simon R. J., Kania R. S., Zuckermann R. N., Huebner V. D., Jewell D. A., Banville S., Ng S., Wang L., Rosenberg S., Marlowe C. K. Peptoids: a modular approach to drug discovery. Proc Natl Acad Sci U S A. 1992 Oct 15;89(20):9367–9371. doi: 10.1073/pnas.89.20.9367. [DOI] [PMC free article] [PubMed] [Google Scholar]
  30. Soothill J. S., Ward R., Girling A. J. The IC50: an exactly defined measure of antibiotic sensitivity. J Antimicrob Chemother. 1992 Feb;29(2):137–139. doi: 10.1093/jac/29.2.137. [DOI] [PubMed] [Google Scholar]
  31. Uttley A. H., Collins C. H., Naidoo J., George R. C. Vancomycin-resistant enterococci. Lancet. 1988 Jan 2;1(8575-6):57–58. doi: 10.1016/s0140-6736(88)91037-9. [DOI] [PubMed] [Google Scholar]
  32. Verhoef J. C., Boddé H. E., de Boer A. G., Bouwstra J. A., Junginger H. E., Merkus F. W., Breimer D. D. Transport of peptide and protein drugs across biological membranes. Eur J Drug Metab Pharmacokinet. 1990 Apr-Jun;15(2):83–93. doi: 10.1007/BF03190191. [DOI] [PubMed] [Google Scholar]
  33. Zasloff M. Antibiotic peptides as mediators of innate immunity. Curr Opin Immunol. 1992 Feb;4(1):3–7. doi: 10.1016/0952-7915(92)90115-u. [DOI] [PubMed] [Google Scholar]

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