Organic anion transporter 1 and Organic anion transporter 3 (OAT1 (SLC22A6), OAT3 (SLC22A8))

Organic anion transporter 1 (OAT1, SLC22A6) and Organic anion transporter 3 (OAT3, SLC22A8) are integral membrane proteins of the solute carrier (SLC) 22 family, primarily expressed on the basolateral membrane of renal proximal tubule cells. They mediate the uptake of a wide array of endogenous organic anions (such as uric acid, prostaglandins, dicarboxylates) and diverse drugs or xenobiotics (including antivirals, antibiotics, NSAIDs, and toxins) from the blood into tubular cells, thereby playing a pivotal role in renal excretion and systemic clearance. OAT1/3 function involves an antiport mechanism with intracellular α-ketoglutarate, itself replenished by sodium-dicarboxylate cotransporters. These transporters are therapeutic targets due to their central role in drug detoxification, renal handling of urate and blood pressure regulators, and are implicated in adverse drug reactions, nephrotoxicity, and variable drug response depending on their activity.

Other names

SLC22A6 (OAT1)SLC22A8 (OAT3)Organic anion transporter family member 1Organic anion transporter family member 3Solute carrier family 22 member 6Solute carrier family 22 member 8

Competitive inhibition of organic anion transport (e.g., probenecid) Inhibition of substrate excretion leading to increased circulating drug/metabolite levels Secondary or tertiary active transport via exchange with α-ketoglutarate, driven by sodium-dependent dicarboxylate uptake