TABLE 3.
Antiviral activity of PIs against recombinant clinical HIV-1 variantsa
| Compound | EC50 (nM) againstb
: |
|||||
|---|---|---|---|---|---|---|
| HIV-1NL4-3c | rCLHIVF16 | rCLHIVT48 | rCLHIVV40 | rCLHIVT44 | rCLHIVM45 | |
| GRL-057-14 | 0.22 ± 0.09 | 0.003 ± 0.001 (0.01) | 0.0005 ± 0.0002 (0.002) | 2.7 ± 1.0 (10) | 0.47 ± 0.47 (2) | 0.07 ± 0.06 (0.3) |
| GRL-058-14 | 9.2 ± 5.3 | 0.01 ± 0.01 (0.001) | 0.18 ± 0.11 (0.02) | 2.1 ± 1.3 (0.2) | 0.6 ± 0.5 (0.06) | 0.52 ± 0.16 (0.05) |
| GRL-059-14 | 10.4 ± 4.4 | 0.47 ± 0.45 (0.05) | 1.8 ± 1.7 (0.2) | 27.3 ± 3.7 (2.7) | 20.5 ± 12.9 (2) | 12.8 ± 3.2 (1.2) |
| APV | 29.4 ± 9.0 | >1,000 (>35) | >1,000 (>35) | 476.4 ± 64.0 (16) | >1,000 (>35) | >1,000 (>35) |
| LPV | 2.4 ± 2.6 | >1,000 (>415) | 290.2 ± 117.9 (120) | 396.0 ± 84.5 (165) | 590.1 ± 38.8 (245) | 426.2 ± 81.7 (175) |
| SQV | 2.5 ± 1.0 | 192.0 ± 205.4 (75) | 210.9 ± 138.0 (85) | >1,000 (>400) | 268.5 ± 40.3 (105) | 252.1 ± 83.7 (100) |
| TPV | 33.2 ± 2.1 | 153.6 ± 3.8 (5) | 235.7 ± 120.3 (7) | 21.7 ± 7.1 (0.7) | 181.5 ± 11.7 (5) | 464.8 ± 100.3 (14) |
| NFV | 32.1 ± 3.2 | 359.4 ± 194.2 (10) | 547.9 ± 134.5 (17) | 254.3 ± 67.4 (8) | 809.3 ± 138.4 (25) | >1,000 (>30) |
| IDV | 25.4 ± 9.8 | 162.0 ± 128.9 (6) | 376.8 ± 40.5 (15) | 438.2 ± 27.1 (17) | 416.9 ± 59.8 (6) | 524.8 ± 80.0 (20) |
| DRV | 3.0 ± 1.0 | 338.4 ± 152.5 (110) | 438.0 ± 239.9 (146) | 11.9 ± 7.8 (4) | 181.5 ± 22.3 (60) | 215.8 ± 91.0 (70) |
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).