Table 1.
Effects of HIV-1 entry inhibitors on CD4-dependent and CD4-independent, CCR5-dependent entrya
| HIV-1 entry inhibitor | Target | Inhibition | Mean EC50 (nM) ± SDb |
|||
|---|---|---|---|---|---|---|
| HeLa CD4/CCR5/CXCR4 |
ACTOne-CCR5 |
|||||
| ADA | ADA S190R/N197S | ADA | ADA S190R/N197S | |||
| BMS-626529 | gp120 | gp120-CD4 interaction | 0.4 ± 0.3 | 0.8 ± 0.1 | No infection | 0.2 ± 0.1 |
| Ibalizumab | CD4 | gp120-coreceptor interaction | 16.6 ± 5.9 | 16.0 ± 1.5 | No infection | >4,950 |
| MVC | CCR5 | gp120-CCR5 interaction | 1.9 ± 0.1 | 0.7 ± 0.7 | No infection | 0.2 ± 0.2 |
| ENF | gp41 | gp41 hairpin formation | 6.5 ± 2.0 | 21.9 ± 7.7 | No infection | 24.1 ± 26.4 |
a
ADA, CD4 dependent, CCR5 dependent; ADA S190R/N197S, CD4 independent, CCR5 dependent; ENF, enfuvirtide; MVC, maraviroc.
b
Mean values of three independent experiments.