MRP2 and 3 in health and disease.
MRPs are membrane proteins transporting organic anions at the expense of ATP hydrolysis. MRP2 is known to be a major transporter of organic anions from the liver into bile. We discuss recent results showing allosteric control of human but not rat MRP2. MRP3 has been considered a major player in bile salt metabolism, but our recent results with Mrp3 KO mice do not support this. Instead, we have found a role for MRP3 in the cellular export of drug-glucuronide conjugates. We discuss problems in extrapolating results obtained for murine MRPs.
Borst
P
P
Division of Molecular Biology, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands. p.borst@nki.nl
Zelcer
N
N
van de Wetering
K
K
D000818:Animals; D001647:Bile Acids and Salts / Q000378:metabolism*; D001692:Biological Transport; D020719:Glucuronides / Q000378:metabolism*; D006801:Humans; D008107:Liver Diseases / Q000378:metabolism* / Q000473:pathology; D026901:Membrane Transport Proteins / Q000502:physiology*; D000089762:Multidrug Resistance-Associated Protein 2; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000502:physiology*
D001647:Bile Acids and Salts; D020719:Glucuronides; D026901:Membrane Transport Proteins; D000089762:Multidrug Resistance-Associated Protein 2; D027425:ATP-Binding Cassette, Sub-Family C Proteins; C000715087:ABCC2 protein, human; C114462:multidrug resistance-associated protein 3