Table 1.
Pyrimidine nucleoside analogues as inhibitors of recombinant human TK2a
| Substrate | Inhibitor | Km (μM) | Ki (μM) |
|---|---|---|---|
| dThd | 1.9 ± 0.2 | ||
| AZT | 3.0 ± 0.3 | ||
| FLT | 1.4 ± 0.2 | ||
| d4T | 24 ± 2.0 | ||
| FIAU | 42.8 ± 5.2 | ||
| FMAU | 8.8 ± 1.0 | ||
| 3TC | 465 ± 12 | ||
| ddC | >1,000 | ||
| dCyd | 11 ± 1.0 | ||
| AZT | >200 | ||
| FLT | >200 | ||
| d4T | >500 | ||
| FIAU | 141 ± 6.0 | ||
| FMAU | 286 ± 12 | ||
| 3TC | 397 ± 9.0 | ||
| ddC | 496 ± 5.0 |
a
Data were from at least three independent measurements performed with variable dThd/dCyd concentrations at three fixed inhibitor concentrations. The Ki values were calculated from plots of slopes of Lineweaver-Burk plots versus inhibitor concentration and are given as means ± standard errors of the means.