Multidrug resistance-associated protein 1 (MRP1) and Multidrug resistance-associated protein 2 (MRP2) (MRP1, MRP2)

Multidrug resistance-associated protein 1 (MRP1, ABCC1) and multidrug resistance-associated protein 2 (MRP2, ABCC2) are members of the ATP-binding cassette (ABC) transporter superfamily, specifically the C subfamily. They function as unidirectional efflux pumps for a broad range of xenobiotics and endogenous compounds, conferring resistance to multiple drugs by actively exporting them out of cells using energy derived from ATP hydrolysis. MRP1 is widely expressed in human tissues (notably blood-tissue barriers, lung, testis, kidney, placenta), while MRP2 is mainly localized to the canalicular membrane of hepatocytes and the apical membrane of renal tubules. Both play important roles in chemo-resistance, the disposition and toxicity of drugs, protection against oxidative stress, and transport of inflammatory and signaling molecules. MRP2 is essential for biliary secretion of organic anions and drugs, and genetic deficiency leads to Dubin–Johnson syndrome. Both transporters are implicated in human disease, especially cancer chemoresistance, and may serve as biomarkers and therapeutic targets[1][2][3][4][5].

Other names

ABCC1ATP-binding cassette sub-family C member 1ABC29GS-XMRPABCC2canalicular multispecific organic anion transporter 1 (cMOAT)ATP-binding cassette sub-family C member 2

ATP-dependent efflux of structurally diverse drugs and metabolites across cellular membranes, reducing cellular drug accumulation and contributing to resistance; Transport of glucuronide, glutathione, and sulfate conjugates; Transport of neutral drugs in complex with glutathione (MRP1/2); Inhibitory drugs may act via direct transporter inhibition, altering drug pharmacokinetics and toxicity profiles