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Multidrug and toxin extrusion transporter 1 (MATE1) is an apically expressed, polyspecific proton/drug antiporter protein primarily found in the brush-border membrane of renal proximal tubule and canalicular membrane of hepatocytes, where it functions to export endogenous and exogenous cations and some anions into urine and bile using an outward proton gradient as the driving force. Encoded by the SLC47A1 gene, MATE1 plays a central role in the renal and hepatic elimination of many drugs, toxins, and metabolites—including metformin, cimetidine, and cisplatin—and is implicated in clinically meaningful drug-drug interactions and inter-individual differences in drug responses. MATE1 is considered a clinically significant transporter for regulatory pharmacokinetic studies and risk assessment[1][4][5][6][7].
Substrate efflux via proton antiport (transports cationic and some anionic drugs/toxins from cells into urine or bile in exchange for protons) Inhibitors block or reduce efflux, altering drug concentrations and contributing to drug-drug interactions
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