Solute carrier family 22 member 6 (hOAT1) and Solute carrier family 22 member 8 (hOAT3) (hOAT1/hOAT3)

Renal organic anion transporters 1 (hOAT1) and 3 (hOAT3) are essential membrane transport proteins located on the basolateral membrane of renal proximal tubule cells. Encoded by the SLC22A6 and SLC22A8 genes, these transporters facilitate the uptake of a diverse array of organic anions from the blood into the tubular cells, representing a critical step in the renal secretion and systemic clearance of both endogenous metabolites and exogenous drugs. They handle a wide variety of substrates, including uremic toxins, signaling molecules like prostaglandins, and numerous therapeutic agents such as beta-lactam antibiotics, nonsteroidal anti-inflammatory drugs (NSAIDs), and antivirals. Because of their broad substrate specificity, hOAT1 and hOAT3 are major sites for drug-drug interactions, where the inhibition of one transporter can significantly alter the pharmacokinetics and toxicity profiles of co-administered medications. Furthermore, these transporters are implicated in drug-induced nephrotoxicity, as the rapid uptake of certain drugs can lead to high intracellular concentrations that damage tubular cells. Consequently, they are recognized by regulatory agencies as key targets for evaluating the safety and interaction potential of new drug candidates.

Other names

SLC22A6SLC22A8Organic anion transporter 1Organic anion transporter 3NKT (Novel Kidney Transporter)PAH transporterPara-aminohippurate transporter

Inhibition of basolateral uptake transporters in the renal proximal tubule, which reduces the secretion of substrate drugs into the urine or prevents the accumulation of nephrotoxic agents within tubular cells.