Table 1. Effect of clotrimazole on kinetics of wild-type OATP1B3 in the absence and presence of the non-transporting OATP1B3-K41C.

Transporter	E17βG			E17βG + 30μM clotrimazole
	Km (μM)	Vmax (pmol/mg protein x min-1)		Km (μM)		Vmax (pmol/mg protein x min-1)
WT-OATP1B3	7.1 ± 0.9	78 ± 3.3		3.3 ± 1.0		107 ± 8.3
WT-OATP1B3 + OATP1B3-K41C	5.5 ± 1.7	48 ± 4.5		3.6 ± 1.3		68 ± 6.5

HEK293 cells were transfected with 500ng of His-tagged OATP1B3 (WT-OATP1B3) or 250ng of His-tagged OATP1B3 plus 250ng of His-tagged OATP1B3-K41C. Kinetic parameters were determined based on the 30 secs uptake of 1, 5, 10, 20, 30 and 50μM E17βG in the absence or presence of 30μM clotrimazole.