TABLE 2.
Susceptibility of selected and gp160-recombined HIV-1 strains to the inhibitory effect of various antiviral compounds
| Compound | EC50a(μg/ml) (fold increase)b
|
||||||
|---|---|---|---|---|---|---|---|
| WT strains
|
Strains resistant to CV-N
|
Strains resistant to ConA
|
Strains with mutated gp120
|
||||
| HIV-1(NL4.3) | R160/NL4.3c | NL4.3/CV-Nresd | R160/CV-Nrese | NL4.3/ConAresd | R160/ConArese | HIV-1(N302K) | |
| Carbohydrate binding inhibitors | |||||||
| CV-N | 0.004 ± 0.002 | 0.003 ± 0.001 | 0.6 ± 0.3 (143) | 0.2 ± 0.01 (77) | 0.6 ± 0.4 (156) | 0.006 ± 0.002 (1.4) | |
| ConA | 2.6 ± 1.4 | 2.2 ± 0.06 | >22.7 ± 1.3 (>8.8) | >23.9 ± 1.0 (>9.3) | >21.5 ± 0.8 (>9.7) | >2.2 ± 0.4 (>0.9) | |
| 2G12 | 0.9 ± 0.2 | 1.0 ± 0.1 | >40 (>43.0) | >40 (>40.0) | >40 (>46.1) | >40 (>40.0) | >40 (>43.0) |
| Reference compounds | |||||||
| AMD3100 | 0.02 ± 0.01 | 0.01 ± 0.008 | 0.03 ± 0.01 (1.3) | 0.02 ± 0.02 (1.4) | 0.03 ± 0.01 (1.5) | 0.02 ± 0.02 (1.7) | 0.009 ± 0.0002 (0.5) |
| Enfuvirtide | 2.1 ± 1.1 | 1.5 ± 0.7 | 3.6 ± 0.9 (1.7) | 2.7 ± 0.8 (1.8) | 3.8 ± 0.3 (1.8) | 3.8 ± 0.7 (2.6) | 2.2 (1.1) |
| Zidovudine | 0.0006 ± 0.0003 | 0.0005 ± 0.0002 | 0.001 ± 0.0004 (1.8) | 0.001 ± 0.0003 (2.6) | 0.001 ± 0.0004 (2.2) | 0.001 ± 0.0004 (2.8) | 0.0004 ± 0.0002 (0.6) |
| Ritonavir | 0.03 ± 0.007 | 0.03 ± 0.002 | 0.04 ± 0.02 (1.4) | 0.03 ± 0.001 (1.2) | 0.04 ± 0.01 (1.4) | 0.04 ± 0.007 (1.4) | 0.02 ± 0.002 (0.6) |
a
50% effective concentration (EC50) or concentration required to inhibit the CPE of different HIV strains by 50% in MT-4 cells.
b
Fold increase in the EC50 of the compound for in vitro-selected HIV-1(NL4.3) or the recombined selected strain compared to the EC50 of the compound for the parental HIV-1(NL4.3) strain or the recombined HIV-1(NL4.3) strain, respectively.
c
HIV-1(NL4.3) wild-type strain recombined with the gp160 gene of pNL4.3.
d
HIV-1(NL4.3) strain selected in vitro in the presence of CV-N or ConA.
e
HIV-1(NL4.3) wild-type strain recombined with the gp160 gene of the respective selected HIV-1(NL4.3) strain.