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- W3173742008 abstract "The human organic cation transporter 2 and human multidrug and toxin extrusion protein 1 (hOCT2/hMATE1) transport system is a pair of transporter proteins highly expressed at the basolateral and apical membrane of renal proximal tubules respectively. They function collaboratively to facilitate elimination of a variety of compounds into urine, thus playing a crucial role in drug disposition and response. Preliminary data from our lab showed that acute exposure (20 minutes) of Cd2+ could significantly upregulate the activities of human hOCT2, while inhibit the function of hMATE1, both in a dose-dependent manner (Fig. 1A&1B). Beside Cd2+, we identified imatinib, an anticancer drug, could induce the function of hOCT2 while inhibit the function of hMATE1 (Fig. 2). In vivo study also showed that pre-treatment of imatinib could significantly increase the accumulation of metformin in mice kidney while had no impact on the plasma exposure of metformin (Fig. 3A&3B). It implicated that the index of plasma drug exposure will not be able to correctly reflect drug-drug interaction when a drug could induce hOCT2 while inhibit hMATE1 at the same time, which potentially could cause significant drug accumulation in kidney tubular cells. Support or Funding Information NIH: R01GM099742FDA: U01FD004320 This abstract is from the Experimental Biology 2018 Meeting. There is no full text article associated with this abstract published in The FASEB Journal." @default.
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- W3173742008 date "2018-04-01" @default.
- W3173742008 modified "2023-10-17" @default.
- W3173742008 title "The Clinical Implication of Compounds which could induce the function of human organic cation transporter 2 (hOCT2), while inhibit the function of human Multidrug and Toxin Extrusion Proteins 1 (hMATE1)" @default.
- W3173742008 doi "https://doi.org/10.1096/fasebj.2018.32.1_supplement.693.7" @default.
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