Solute carrier family 22 member 6 (OAT1) (OAT1)

Solute carrier family 22 member 6, commonly known as Organic Anion Transporter 1 (OAT1), is a transmembrane protein primarily expressed in the basolateral membrane of renal proximal tubule cells (UniProt: Q4U2R8). It functions as an organic anion/dicarboxylate exchanger, playing a critical role in the renal secretion of a wide range of endogenous metabolites, such as alpha-ketoglutarate, and exogenous compounds, including many clinically important drugs (PubMed: 24338212). OAT1 is a major determinant of the pharmacokinetics and systemic clearance of various antibiotics, antivirals, and anti-inflammatory agents (NCBI Gene: 9356). Because it facilitates the entry of potentially toxic substances into renal cells, it is a key mediator of drug-induced nephrotoxicity, particularly for drugs like cidofovir and tenofovir (PubMed: 15102893). Consequently, OAT1 is a significant focus in drug development for assessing drug-drug interactions and predicting renal safety profiles (FDA Guidance, 2020). Its activity can be modulated by inhibitors like probenecid, which are sometimes used therapeutically to reduce the renal clearance of other drugs or protect the kidneys from toxicity.

Other names

Organic anion transporter 1SLC22A6PAHTROAT1NKTmOat1

OAT1 facilitates the uptake of organic anions from the peritubular capillaries into renal proximal tubule cells via an exchange mechanism with intracellular dicarboxylates like alpha-ketoglutarate. Drugs can act as substrates for this transport, leading to their renal excretion, or as inhibitors that block the transport of other substances, thereby modulating their plasma concentration or preventing cellular toxicity (PubMed: 24338212).