Table 5.
Antiviral activity of 2 and 22 against highly PI-resistant HIV-1 variants.
| Mean IC50 in nM ± SD (fold-change) | ||||||
|---|---|---|---|---|---|---|
| Virus Species | LPV | ATV | DRV | 22 (GRL-121) | 2 (GRL-142) | |
| cHIVnl4–3WT | 13 ± 2 | 4.0 ± 2.3 | 3.2 ± 0.7 | 0.26 ± 0.05 | 0.019 ± 0.017 | |
| HIVSQV-5μM | >1000 (>77) | 430 ± 20 (108) | 17 ± 7 (5) | 0.026 ± 0.01 (0.1) | 0.00018 ± 0.00003 (0.009) | |
| HIVAPV-5μM | 280 ± 15 (22) | 3.0 ± 1.0 (1) | 39 ± 16 (12) | 0.13 ± 0.08 (0.5) | 0.0000085 ± 0.000008 (0.0004) | |
| HIVLPV-5μM | >1000 (>77) | 46 ± 10 (12) | 280 ± 50 (86) | 0.0018 ± 0.001 (0.007) | 0.000019 ± 0.0000014 (0.0001) | |
| HIVIDV-5μM | 250 ± 15 (19) | 56 ± 9 (14) | 37 ± 8 (12) | 0.0092 ± 0.016 (0.04) | 0.00018 ± 0.00028 (0.009) | |
| HIVNFV-5μM | 37 ± 3 (3) | 12 ± 2 (3) | 7.7 ± 3 (2) | 0.048 ± 0.02 (0.2) | 0.00024 ± 0.00026 (0.01) | |
| HIVATV-5μM | 310 ± 20 (24) | >1000 (>250) | 25 ± 1 (8) | 0.092 ± 0.09 (0.4) | 0.015 ± 0.004 (0.8) | |
| HIVTPV-15μM | >1000 (>77) | >1000 (>250) | 40 ± 3 (13) | 0.063 ± 0.02 (0.2) | 0.00024 ± 0.00007 (0.01) | |
*
invitroHIVPIR, in vitro PI-selected HIV-1 variants;
**
rCLHIV, recombinant clinical HIV-1 variants. Numbers in parentheses represent fold changes in IC50s for each isolate compared to the IC50s for wild-type cHIVNL4–3WT. All assays were conducted in triplicate, and the data shown represent mean values (±1 standard deviation) derived from the results of three independent experiments. DOI: https://doi.org/10.7554/eLife.28020.005