TABLE 3.
Ki and Ki/Km of wild-type and mutant HIV-1 RT enzymes
| HIV-1 RT | Tenofovir-PP
|
ddATP
|
Carbovir-TP
|
DXG-TP
|
||||
|---|---|---|---|---|---|---|---|---|
| Ki (μM)a (fold)b | Ki/Km (fold)c | Ki (fold) | Ki/Km (fold) | Ki (μM) (fold) | Ki/Km (fold) | Ki (μM) (fold) | Ki/Km (fold) | |
| Wild type | 0.155 (1.0) | 0.46 (1.0) | 0.024 (1.0) | 0.072 (1.0) | 0.181 (1.0) | 1.05 (1.0) | 0.008 (1.0) | 0.05 (1.0) |
| K65R | 1.040d (6.7) | 2.67 (5.8) | 0.173e (7.2) | 0.441 (6.1) | 0.357 (2.0) | 1.42 (1.3) | 0.033e (4.1) | 0.13 (2.8) |
| K65R+M184V | 0.824d (5.3) | 1.62 (3.5) | 0.383d (16) | 0.690 (9.6) | 0.807d (4.5) | 2.45 (2.3) | 0.033e (4.1) | 0.10 (2.2) |
Ki values are averages for three to six experiments, with average standard errors of 0.067 for tenofovir-PP, 0.013 for ddATP, 0.059 for carbovir-TP, and 0.003 for DXG-TP.
Fold change in Ki value from that for the wild type.
Fold change in Ki/Km value from that for the wild type.
P < 0.001 compared to the Ki for the wild type by two-tailed Student's t test.
P < 0.05 compared to the Ki for the wild type by two-tailed Student's t test.