TABLE 4.
Antiviral activity of PIs against HIV-1 variants carrying single amino acid substitutionsa
| Compound | EC50 (nM) againstb
: |
|||
|---|---|---|---|---|
| HIV-1NL4-3c | rHIVL24M | rHIVR41T | rHIVK55N | |
| GRL-057-14 | 0.22 ± 0.09 | 0.00000035 ± 0.00000021 (0.000002) | 0.00015 ± 0.00021 (0.0007) | 0.000006 ± 0.000002 (0.00003) |
| GRL-058-14 | 9.2 ± 5.3 | 0.2 ± 0.03 (0.02) | 2.0 ± 1.1 (0.2) | 6.3 ± 1.8 (0.7) |
| GRL-059-14 | 10.4 ± 4.4 | 18.5 ± 2.1 (1.8) | 2.0 ± 0.5 (0.2) | 4.5 ± 2.7 (0.4) |
| DRV | 3.0 ± 1.0 | 3.0 ± 1.0 (1.0) | 2.7 ± 1.5 (0.9) | 1.3 ± 0.01 (0.4) |
a
Anti-HIV-1 activity was determined with a p24 assay employing MT-4 cells. Each assay was conducted in triplicate. The values represent mean values (±1 SD) of two or three independent experiments. Numbers in parentheses represent fold changes in EC50s for each isolate compared to the EC50s for wild-type HIV-1NL4-3.
b
EC50, 50% effective concentration.
c
Data from Table 2 (HIV-1NL4-3).