Table 2. Effect of selected compounds on the HIV-1 RT associated RNase H function of mutated RTs.
|
A
|
AA
|
AB
|
BTP |
|||||
| IC50 a (μM) | Fold b | IC50 a (μM) | Fold b | IC50 a (μM) | Fold b | IC50 a (μM) | Fold b | |
| Wild | 9.35 ± 0.73 | — | 5.1 ± 1.89 | — | 12.82 ± 1.05 | — | 0.20± 0.02 | — |
| A502F | 32.52 ± 2.83 | 3.5*** | 26.72 ± 3.14 | 5.3*** | 26.35 ± 1.01 | 2.1**** | 0.17 ± 0.03 | 0.85 |
| R557A | 20.54 ± 1.26 | 2.2*** | 12.53 ± 1.36 | 2.5** | 18.61 ± 0.42 | 1.5** | 0.21 ± 0.05 | 1.05 |
| R448A | 10.96 ± 1.12 | 1.20 | 7.01 ± 0.78 | 1.40 | 11.28 ± 0.64 | 0.9 | 0.14 ± 0.02 | 0.70 |
| N474A | >300 | >32**** | >300 | >59**** | 146 ± 12 | 11.4**** | 0.10 ± 0.01 | 0.50 |
aConcentration required to inhibit HIV-1 RT-associated RNase H activity by 50% obtained by three independent experiments (reported as average ± standard deviation). p value < 0.05 (*); p value < 0.01 (**); p value < 0.001 (***); p value < 0.0001(****).
bFold of increase with respect to WT RT.