Canalicular multispecific organic anion transporter 1 (MRP2) (MRP2)

Canalicular multispecific organic anion transporter 1, commonly known as Multidrug resistance-associated protein 2 (MRP2), is an ATP-dependent efflux pump encoded by the ABCC2 gene (UniProt: P51442). It is primarily localized to the canalicular membrane of hepatocytes, where it facilitates the excretion of conjugated organic anions, such as bilirubin glucuronides and glutathione conjugates, into the bile (PubMed: 10510306). Beyond the liver, it is expressed in the kidneys and intestines, influencing the absorption and elimination of various xenobiotics. Mutations in the ABCC2 gene cause Dubin-Johnson syndrome, a condition marked by conjugated hyperbilirubinemia due to impaired biliary secretion (StatPearls: Dubin-Johnson Syndrome). In oncology, MRP2 is a significant factor in multidrug resistance, as it can efflux chemotherapeutic agents like cisplatin and methotrexate out of tumor cells (PubMed: 21114571). Additionally, it is a key site for drug-drug interactions, as many drugs act as substrates or inhibitors, potentially leading to altered pharmacokinetics and toxicity.

Other names

Multidrug resistance-associated protein 2ABCC2cMOATATP-binding cassette sub-family C member 2

ATP-dependent efflux of endogenous and exogenous organic anions across the canalicular membrane of hepatocytes into the bile (UniProt: P51442).