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Human organic anion transporter 1 (OAT1), encoded by the SLC22A6 gene, is a transmembrane protein primarily expressed on the basolateral membrane of proximal tubular cells in the kidneys. It mediates the uptake and exchange of a wide range of small, hydrophilic organic anions from plasma into renal tubular cells for subsequent excretion into urine. This process is essential for clearing endogenous metabolites as well as various drugs from circulation. OAT1 functions as part of a coordinated system with other transporters such as NaDC3, which replenishes intracellular dicarboxylates required for its activity. The protein belongs to both the solute carrier family and major facilitator superfamily. Its function is critical in pharmacokinetics—alterations can lead to significant changes in drug disposition, efficacy, toxicity risk, and susceptibility to nephrotoxic injury.
Inhibition of OAT1-mediated transport to alter renal clearance or tissue distribution of drugs/metabolites
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