TABLE 2

Kinetic parameters of glyburide transport in HEK cells overexpressing BCRP protein (WT or C421A)a

Genistein (µM)
0210
WT-BCRP
 Km (µM)70.5 ± 17.012.1 ± 6.59b1.0 ± 0.19b
 Jmax (pmol 3H-glyburide/mg protein)0.69 ± 0.170.68 ± 0.120.89 ± 0.23
C421A-BCRP
Km (µM)14.5 ± 1.48c2.52 ± 1.84b0.61 ± 0.22b
Jmax (pmol 3H-glyburide/mg protein)0.73 ± 0.210.79 ± 0.110.82 ± 0.14
  • a Km and Jmax values were calculated using Graphpad nonlinear regression analysis (Michaelis-Menten) and are presented as mean ± S.D. (n = 3 independent experiments).

  • b P < 0.05 compared with 0 µM genotype control.

  • c P < 0.05 compared with 0 µM WT-BCRP control.