Canalicular multispecific organic anion transporter 1 (MRP2)

Canalicular multispecific organic anion transporter 1, commonly known as Multidrug resistance-associated protein 2 (MRP2), is a vital member of the ATP-binding cassette (ABC) transporter superfamily. It is primarily expressed on the canalicular membrane of hepatocytes, where it mediates the ATP-dependent secretion of organic anions, including bilirubin glucuronides and glutathione conjugates, into the bile (UniProt Q92887). Beyond the liver, MRP2 is found in the kidneys and intestines, playing a significant role in the renal excretion and limiting the absorption of various xenobiotics (PubMed: 11470988). Genetic mutations in the ABCC2 gene result in Dubin-Johnson syndrome, a condition characterized by chronic conjugated hyperbilirubinemia (NIH: GARD). In the context of oncology, MRP2 is frequently overexpressed in various tumors, contributing to multidrug resistance by actively effluxing chemotherapeutic agents such as cisplatin and methotrexate (PubMed: 15121053). Understanding MRP2 function is essential for predicting drug-drug interactions and optimizing the therapeutic efficacy of drugs that are substrates for this transporter.

Other names

Multidrug resistance-associated protein 2ATP-binding cassette sub-family C member 2ABCC2Canalicular multispecific organic anion transporter 1cMOAT

MRP2 functions as an ATP-dependent efflux pump that actively transports a broad range of endogenous and exogenous substrates, particularly organic anions and their phase II conjugates, across the apical membrane of polarized cells into the bile, urine, or intestinal lumen (UniProt Q92887).