SLCO1A2 Gene - Organic Anion Transporting Polypeptide 1A2 (OATP1A2)

SLCO1A2 encodes the organic anion transporting polypeptide 1A2 (OATP1A2), a sodium-independent transmembrane transporter. It is primarily expressed on the basolateral membrane of hepatocytes, renal proximal tubule cells, and brain capillary endothelial cells. OATP1A2 mediates the cellular uptake of a wide range of endogenous compounds (e.g., bile acids, bilirubin, steroid hormones) and xenobiotics (e.g., statins, antibiotics, anticancer drugs). Genetic variants in SLCO1A2 can alter transporter activity and influence drug pharmacokinetics and toxicity.

Tissue Expression

Cell Line Expression

Hotspot Mutations

Mutation functional classification

• REACT:111045 – Bile acid and bile salt metabolism

• REACT:155581 – Transport of organic anions

• REACT:156588 – Drug ADME

OATP1A2 is a 670-amino acid transmembrane protein with 12 predicted membrane-spanning domains. It functions as a sodium-independent organic anion exchanger, coupling the uptake of substrates with the efflux of intracellular anions such as glutathione or bicarbonate. The protein is glycosylated and localized to the basolateral membrane of polarized cells. OATP1A2 exhibits broad substrate specificity, including bile acids, steroid conjugates, thyroid hormones, and numerous drugs (e.g., fexofenadine, methotrexate, rosuvastatin).