TABLE 1.
Inhibition of HIV-1 Env variants by CD4-mimetic compounds and the 17b CD4i antibody
| Virus | Clade | IC50 of: |
||||
|---|---|---|---|---|---|---|
| 17ba (μg/ml) | 17b + 50 μM BNM-III-170a (μg/ml) | 17b + 50 μM BNM-IV-147a (μg/ml) | BNM-III-170b (μM) | BNM-IV-147b (μM) | ||
| JR-FL wt | B | >30 | 0.2 ± 0.0 | 0.2 ± 0.0 | 18.9 ± 3.8 | 6.7 ± 0.9 |
| JR-FL S375W | B | >30 | >30 | >30 | >100 | 90.5 |
| YU2 wt | B | >30 | 0.2 ± 0.1 | 0.1 | 1.2 ± 0.1 | 0.4 |
| YU2 S375W | B | >30 | >30 | >30 | >100 | 88.7 |
| YU2 S375A | B | >30 | 0.2 ± 0.0 | 0.4 | 0.6 ± 0.0 | 0.4 |
| A4 | A | >30 | 1.6 ± 0.8 | 11.0 ± 6.7 | 4.5 ± 1.4 | 1.8 ± 0.4 |
| B6 | B | >30 | >30 | >30 | 47.6 ± 19.0 | 15.8 ± 1.4 |
| C5 | C | >30 | 5.7 ± 4.8 | 17.2 ± 8.5 | 9.2 ± 2.7 | 5.9 ± 2.1 |
| C11 | C | >30 | >30 | >30 | 36.6 ± 8.4 | 14.4 ± 0.3 |
| C17 | C | >30 | >30 | 20.1 ± 9.9 | 7.4 ± 0.6 | 4.4 ± 0.9 |
| 821 | D | >30 | 1.5 ± 1.2 | 12.8 ± 8.3 | 0.5 ± 0.0 | 0.5 ± 0.0 |
| 859 | D | >30 | 19.2 ± 9.6 | 10.3 ± 9.9 | 2.5 ± 0.2 | 1.1 ± 0.2 |
| AG266 | AG Subtype | >30 | >30 | 12.9 ± 8.8 | 25.2 ± 1.5 | 7.7 ± 0.2 |
| A-MLV | >30 | 25.5 ± 4.5 | >30 | 88.7 ± 11.2 | 81.2 ± 9.4 | |
Recombinant HIV-1 encoding firefly luciferase was pseudotyped with the indicated HIV-1 Env (or A-MLV Env control). Viruses were incubated with 50 μM CD4-mimetic compound (BNM-III-170 or BNM-IV-147) or with DMSO and then with different concentrations of the 17b antibody. After incubation of the viruses with Cf2Th-CD4/CCR5 cells for 48 h, the cells were lysed and luciferase activity was measured. The inhibitory concentration (IC50) of the 17b antibody is reported. Means and standard deviations from triplicate samples within an experiment are shown. ND, not determined.
The inhibitory concentrations (IC50) for the direct antiviral effect of BNM-III-170 and BNM-IV-147 were determined as in footnote a.