Kinetic parameters of ACV, GCV, and AZT uptake by hOATs and by hOCTs
| ACV | GCV | AZT | |||||||
|---|---|---|---|---|---|---|---|---|---|
| Km | Vmax | Km/Vmax | Km | Vmax | Km/Vmax | Km | Vmax | Km/Vmax | |
| hOAT1 | 342.3 ± 53.4 | 1275.9 | 3.73 | 895.5 ± 99.4 | 1165.5 | 1.30 | 45.9 ± 5.98 | 254.6 | 5.53 |
| hOAT2 | 26.8 ± 2.58 | 106.8 | 3.99 | ||||||
| hOAT3 | 145.1 ± 13.2 | 757.7 | 5.22 | ||||||
| hOAT4 | 151.8 ± 10.2 | 367.1 | 2.42 | ||||||
| hOCT1 | 151.2 ± 22.1 | 133.4 | 0.88 | 516.2 ± 70.3 | 200.3 | 0.388 | |||
| hOCT2 | |||||||||
S2 hOAT1, S2 hOAT2, S2 hOAT3, S2 hOAT4, S2 hOCT1, S2 hOCT2, and S2 pcDNA 3.1 were incubated in solution containing various concentrations of either [3H]ACV, [3H]GCV, or [3H]AZT at 37°C for 1 min. The uptake in mock was subtracted. Units of Km,Vmax, andKm/Vmax values are μM, pmol/mg of protein/min and μl/mg of protein/min, respectively. Each value represents the mean of three determinations from one typical experiment.