Table 2

Kinetic parameters of ACV, GCV, and AZT uptake by hOATs and by hOCTs

ACVGCVAZT
KmVmaxKm/VmaxKmVmaxKm/VmaxKmVmaxKm/Vmax
hOAT1342.3 ± 53.41275.93.73895.5 ± 99.41165.51.3045.9 ± 5.98254.65.53
hOAT226.8 ± 2.58106.83.99
hOAT3145.1 ± 13.2757.75.22
hOAT4151.8 ± 10.2367.12.42
hOCT1151.2 ± 22.1133.40.88516.2 ± 70.3200.30.388
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.