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Solute carrier family 22 member 7 (OAT2) is a multispecific organic anion transporter primarily expressed in the liver and kidney (UniProt P48431). It plays a critical role in the disposition of various endogenous compounds, such as creatinine and cyclic nucleotides, as well as a wide range of clinically important drugs including antivirals and chemotherapeutics (PMID: 24515016). In the liver, OAT2 is located on the sinusoidal membrane, facilitating the uptake of substrates from the blood, while in the kidney, it is found on the basolateral membrane of proximal tubule cells (PMID: 15970509). Because it handles many common medications, OAT2 is a significant site for drug-drug interactions, where competition for the transporter can lead to altered plasma concentrations and potential toxicity (FDA Drug Development and Drug Interactions Guidance). Understanding OAT2's function is essential for predicting the pharmacokinetics and safety profiles of new therapeutic agents, particularly those cleared via renal or hepatic pathways. Additionally, OAT2 has been identified as a major transporter for the entry of the chemotherapy drug 5-fluorouracil into hepatocytes, influencing its metabolic activation and systemic clearance (PMID: 15970509).
Substrate transport via facilitated diffusion and secondary active transport; competitive and non-competitive inhibition by drugs
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