A Family of Drug Transporters: the Multidrug Resistance-Associated Proteins

摘要: The human multidrug resistance-associated protein (MRP) family currently has seven members. ability of several these membrane proteins to transport a wide range anticancer drugs out cells and their presence in many tumors make them prime suspects unexplained cases drug resistance, although proof that they contribute clinical resistance is still lacking. Recent studies have begun clarify the function MRP MRPs are organic anion transporters; i.e., anionic drugs, exemplified by methotrexate, neutral conjugated acidic ligands, such as glutathione (GSH), glucuronate, or sulfate. However, MRP1, MRP2, MRP3 can also cause not known be ligands transporting together with free GSH. MRP1 even confer arsenite MRP2 cisplatin, again probably compounds complexes MRP4 overexpression associated high-level nucleoside analogues 9-(2-phosphonylmethoxyethyl) adenine azidothymidine, both which used anti-human immunodeficiency virus drugs. may, therefore, role against cancer chemotherapy. Mice without Mrp1, high-affinity leukotriene C(4) transporter, an altered response inflammatory stimuli but otherwise healthy fertile. major transporter responsible for secretion bilirubin glucuronides into bile, humans develop mild liver disease Dubin-Johnson syndrome. physiologic functions other known. Whether long-term inhibition tolerated (assuming suitable inhibitors will found) remains determined.