Double-transduced MDCKII cells to study human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) interplay in drug transport across the blood-brain barrier.
作者： Birk Poller , Els Wagenaar , Seng Chuan Tang , Alfred H. Schinkel
DOI: 10.1021/MP1003898
关键词:
摘要: P-glycoprotein (P-gp/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) combination knockout mice display disproportionately increased brain penetration of shared substrates, including topotecan several tyrosine kinase inhibitors, compared to deficient for only one transporter. To better study the interplay both transporters also in vitro, we generated a transduced polarized MDCKII cell line stably coexpressing substantial levels human ABCB1 ABCG2 (MDCKII-ABCB1/ABCG2). Next, measured concentration-dependent transepithelial transport topotecan, sorafenib sunitinib. By blocking either or simultaneously, using specific aimed mimic ABCB1-ABCG2 at blood−brain barrier wild-type, single mice. contributed similar extents transport, which was partly saturable. For major determinant low concentrations. However, satur...
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