Inhibitory activity of test compounds against mutant HIV-1 RTs (N136X)
Data are the mean (± S.D.) of at least three to four independent experiments.
| RT Mutation | IC50 | ||||
|---|---|---|---|---|---|
| Nevirapine | Delavirdine | Efavirenz | Quinoxaline | ddGTP | |
| μM | |||||
| WT | 0.45 ± 0.25 | 0.31 ± 0.025 | 0.027 ± 0.006 | 0.022 ± 0.006 | 0.051 ± 0.009 |
| N136T | 1.0 ± 0.29 | 0.90 ± 0.16 | 0.035 ± 0.006 | 0.033 ± 0.004 | 0.065 ± 0.007 |
| N136A | >10 | 6.6 ± 2.4 | 0.21 ± 0.20 | 0.28 ± 0.01 | 0.28 ± 0.48 |
| N136Q | ≥10 | 4.5 ± 1.7 | 0.051 ± 0.018 | 0.39 ± 0.21 | 1.4 ± 0.20 |
| N136S | 5.1 ± 2.6 | 3.1 ± 1.7 | 0.052 ± 0.044 | 0.35 ± 0.32 | 0.58 ± 0.51 |
| N136K | >10 | ≥10 | 0.16 ± 0.021 | ≥1 | 0.93 ± 0.64 |
| N136L | >10 | 9.1 ± 1.3 | 0.13 ± 0.014 | 0.80 ± 0.021 | 6.1 ± 1.0 |
| N136D | 2.7 ± 2.3 | 1.3 ± 1.2 | 0.036 ± 0.0007 | 0.037 ± 0.002 | 0.19 ± 0.021 |
| N136Y | >10 | >10 | 0.12 ± 0.01 | ≥1 | 1.6 ± 0.32 |
Template/primer, poly(rC) · oligo(dG); substrate, 1.6 μM [3H]dGTP.