TABLE 2.
Kinetic parameters of BAC C8 and BAC C10 uptake by hOCT1–3 and hMATE1/2K
Models were chosen based on examination of Eadie-Hofstee plots. The standard Michaelis-Menten equation (eq. 2) was fitted to the BAC C8 data, whereas a substrate-inhibition model (eq. 3) was fitted to the BAC C10 uptake kinetics. Results are represented as mean ± S.D. of the Km, Vmax, and Ki,[s] from three independent experiments.
| Transporter | BAC C8 | BAC C10 | |||
|---|---|---|---|---|---|
| Km (μM) |
Vmax (pmol/mg protein/min) |
Km (μM) |
Vmax (pmol/mg protein/min) |
Ki,[s] (μM) |
|
| hOCT1 | 8.7 ± 2.3 | 1091 ± 339 | 6.8 ± 3.8 | 1480 ± 163 | 93.1 ± 19.4 |
| hOCT2 | 10.4 ± 3.9 | 965 ± 43 | 19.1 ± 6.8 | 2673 ± 412 | 106.5 ± 11.2 |
| hOCT3 | 18.9 ± 2.4 | 1716 ± 157 | 27.4 ± 22.1 | 2421 ± 1233 | 37.1 ± 19.3 |
| hMATE1 | 6.0 ± 0.7 | 487 ± 206 | 4.9 ± 1.4 | 975 ± 49 | 52.2 ± 16.2 |
| hMATE2K | 9.7 ± 4.1 | 2239 ± 385 | 19.3 ± 0.3 | 6102 ± 973 | 111 ± 27.6 |