Table IV. Inhibition of wild-type and drug-resistant HIV-1 reverse transcriptase by nucleotide analogues.
| Reverse transcriptase | Wild type | R72A | K65A | K65R |
|---|---|---|---|---|
| Relative catalytic efficiencya | 1 | 0.04 | 0.46 | 0.96 |
| AZT triphosphate | ||||
| Ki (nM)b | 21.8 | 6500 | 125 | 20.5 |
| α-borano Ki (nM)b | 8.25 | 32.5 | 9 | 9 |
| Ratio | 2.6 | 200 | 13.9 | 2.2 |
| d4T triphosphate | ||||
| Ki (nM)b | 49.2 | 500 | 275 | 60 |
| α-borano Ki (nM)b | 20.3 | 5 | 27.5 | 19.5 |
| Ratio | 2.4 | 100 | 10 | 3 |
aOligo(dT)12–18–poly(rA) primer–template, TTP as the nucleotide substrate (Ueno et al., 1995). The catalytic efficiency is measured relative to wild-type reverse transcriptase (0.63 µM–1s–1).
bThese Ki values were determined as described (Ueno et al., 1995), from three and two independent experiments for wild-type and variant reverse transcriptases, respectively.