Mrp2 - cynomolgus monkey New
Mrp2 (multidrug resistance-associated protein 2), cynomolgus monkey
Gene name: ATP binding cassette subfamily C member 2 (Abcc2)
Human MRP2 (multidrug resistance-associated protein 2) is a unidirectional efflux transporter that primarily transports organic anions, organic anion conjugates and other substrates across cell membranes. It is a full transporter localized on the apical membrane of polarized cells in various tissues and barriers, including the kidney, the liver and the intestine. MRP2 transports conjugated endogenous and xenobiotic substances, including hormones, toxins and carcinogens, into the bile (from hepatocytes), urine (from renal proximal tubular cells), and the intestinal lumen (from enterocytes). The MRP2 membrane protein, like the most ABC transporters, transports substrates across the cell membrane using ATP as an energy source.
The cynomolgus monkey (Macaca fascicularis), as a nonhuman primate, is generally considered as a superior model for human drug disposition, and has consequently become a key preclinical species in drug development. The amino acid sequence encoded by monkey MRP2 cDNA is reported to very similar (96% identity) to the human MRP2 cDNA. E217βG exhibited a higher affinity for monkey MRP2 compared to human MRP2.
A simple method for measuring cyMrp2-mediated transport in vitro is the vesicular transport (VT) assay. The interaction is detected as the modulation of the initial rate of [3H]-E217βG transport by cyMrp2 into inside-out membrane vesicles, which were purified from HEK293 cells expressing cyMrp2 transporter.
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