Figure 8.

ABCC10 and ABCG2-mediated transport of gefitinib in vitro. (A,B) Characterization of the LLC-PK1 cell line overexpression human ABCC10 or ABCG2. mRNA and protein levels of human ABCC10 or ABCG2 were detected in wildtype LLC-PK1 (LLC-WT) cells, as well as its subclones transduced with human ABCC10 (LLC-ABCC10) or ABCG2 (LLC-ABCG2). **P < 0.01 compared with LLC-WT cells. (C), Transepithelial transport of 100 nmol/L [³H]-paclitaxel and 10 nmol/L [³H]-estrone-3-sulfate in LLC-WT, LLC-ABCC10, and LLC-ABCG2 cells. At t = 0 h, [³H]-paclitaxel or [³H]-estrone-3-sulfate was applied in one compartment (apical or basal). At t = 4 h, the radioactivities were measured and the efflux ratios (ERs) were caluculated. **P < 0.01 compared with LLC-WT cells. (D) Transepithelial transport of 100 nmol/L [³H]-gefitinib was assessed in LLC-PK1 cells. At t = 0 h, [³H]-gefitinib was applied in one compartment (apical or basal), and the radioactivities at t = 2, 4, and 6 h were measured and plotted over time. Closed circles, translocation from the basal to the apical compartment; open circles, translocation from the apical to the basal compartment. *P < 0.05, **P < 0.01 compared to the translocation from the apical to the basal compartment.