Solute carrier family 22 member 6 and Solute carrier family 22 member 8 (OAT1 and OAT3)

Human organic anion transporters 1 (OAT1, SLC22A6) and 3 (OAT3, SLC22A8) are essential multispecific transporters located on the basolateral membrane of renal proximal tubule cells [1.2.1, 1.3.2]. They mediate the rate-limiting step in the renal secretion of a diverse array of small, negatively charged molecules, including endogenous metabolites, uremic toxins, and clinically significant drugs [1.1.2, 1.3.3]. These transporters function via a tertiary active transport mechanism, where the uptake of an organic anion is coupled to the efflux of an intracellular dicarboxylate, such as alpha-ketoglutarate [1.2.3, 1.3.1]. OAT1 and OAT3 are critical determinants of the pharmacokinetics and safety profiles of many drugs, including antibiotics, antivirals like tenofovir, and nonsteroidal anti-inflammatory drugs (NSAIDs) [1.2.2, 1.4.1]. Because they share many substrates, they are frequent sites of clinically relevant drug-drug interactions; for example, the inhibitor probenecid is often used to reduce the renal clearance of co-administered drugs [1.2.3, 1.3.5]. Beyond their role in drug handling, they are involved in maintaining systemic homeostasis and are implicated in the Remote Sensing and Signaling hypothesis, which suggests they facilitate interorgan communication by regulating levels of signaling molecules [1.1.5, 1.3.1]. Dysregulation or inhibition of these transporters is associated with conditions such as chronic kidney disease, hypertension, and drug-induced nephrotoxicity [1.1.3, 1.3.2, 1.4.2].

Other names

hOAT1hOAT3SLC22A6SLC22A8Organic anion transporter 1Organic anion transporter 3Novel kidney transporter (NKT)p-aminohippurate transporter (PAHT)Renal organic anion transporter 1 (ROAT1)HOAT1HOAT3

Tertiary active transport involving the exchange of intracellular dicarboxylates (e.g., alpha-ketoglutarate) for extracellular organic anions [1.2.3, 1.3.1].