TABLE 2.
Kinetic parameters of glyburide transport in HEK cells overexpressing BCRP protein (WT or C421A)a
|
Genistein (µM) |
|||
|---|---|---|---|
| 0 | 2 | 10 | |
| WT-BCRP | |||
| Km (µM) | 70.5 ± 17.0 | 12.1 ± 6.59b | 1.0 ± 0.19b |
| Jmax (pmol 3H-glyburide/mg protein) | 0.69 ± 0.17 | 0.68 ± 0.12 | 0.89 ± 0.23 |
| C421A-BCRP | |||
| Km (µM) | 14.5 ± 1.48c | 2.52 ± 1.84b | 0.61 ± 0.22b |
| Jmax (pmol 3H-glyburide/mg protein) | 0.73 ± 0.21 | 0.79 ± 0.11 | 0.82 ± 0.14 |
Km and Jmax values were calculated using Graphpad nonlinear regression analysis (Michaelis-Menten) and are presented as mean ± S.D. (n = 3 independent experiments).
P < 0.05 compared with 0 µM genotype control.
P < 0.05 compared with 0 µM WT-BCRP control.