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Organic anion transporter 1 and Organic anion transporter 3 are high-capacity, multispecific transport proteins of the SLC22 family, mainly expressed in the basolateral membrane of renal proximal tubule cells. They mediate the secondary active uptake of a wide range of endogenous metabolites, environmental toxins, and therapeutic drugs from the blood into kidney cells. Inside the cell, these compounds are subsequently extruded into the urine via other transporters and excreted from the body. Their function is essential for drug clearance, renal homeostasis, and systemic detoxification. Dysfunction or pharmacological inhibition of these transporters can have profound effects on drug efficacy, toxicity, and the progression of renal diseases.
Antiport mechanism: organic anion uptake exchanged for intracellular dicarboxylates (e.g., α-ketoglutarate). Substrate translocation from blood to intracellular compartment, facilitating excretion.
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