Biochemical Pharmacology volume 80, issue 7, P1087-1092 2010 DOI: 10.1016/j.bcp.2010.06.012 View full text
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Xiaowan Zheng, Lei Diao, Sean Ekins, James E. Polli

Abstract: AbstractFrom routine in vitro drug-transporter inhibition assays, observed inhibition is typically assumed from direct interaction with the transporter. Other mechanisms that possibly reduce substrate uptake are not frequently fully examined. The objective of this study was to investigate the association of transporter inhibition with drug cytotoxicity. From a pool of drugs that were identified as known ASBT or OCTN2 inhibitors, twenty one drugs were selected to screen inhibitory potency of their prototypical…

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