TABLE 1.
Kinetic parameters for binding of efavirenz, sefavirenz, and nevirapine to different catalytic forms of HIV-1 RT
Drug | Catalytic form | Mean ± SD
|
|||
---|---|---|---|---|---|
Kd (nM) | kapp (s−1) | kon (s−1 M−1)a | koff (s−1)b | ||
Efavirenz | RT | 170 ± 5 | NAc | NA | NA |
RT-TPd | 30 ± 2 | (6 ± 1) × 10−3 | (1.3 ± 0.2) × 104 | (4 ± 1) × 10−4 | |
RT-TP-dNTPe | 4 ± 0.5 | (7 ± 1) × 10−3 | (3.4 ± 0.2) × 104 | (1.6 ± 0.5 × 10−4 | |
Sefavirenz | RT | 750 ± 15 | NA | NA | NA |
RT-TPd | 230 ± 20 | (4 ± 1) × 10−3 | (0.5 ± 0.1) × 104 | (1 ± 0.5) × 10−3 | |
RT-TP-dNTPe | 8 ± 0.5 | (6 ± 1) × 10−3 | (5.5 ± 0.5) × 104 | (4 ± 1) × 10−4 | |
Nevirapine | RT | 400 ± 15 | NA | NA | NA |
RT-TPd | 400 ± 20 | (5.7 ± 1) × 10−3 | (0.15 ± 0.03) × 104 | (6 ± 0.5) × 10−4 | |
RT-TP-dNTPe | 450 ± 25 | (6 ± 1) × 10−3 | (0.2 ± 0.05) × 104 | (6 ± 1) × 10−4 |
Calculated from kapp = kon (Ki + [I]).
Calculated from Kd = koff/kon.
NA, not applicable.