The multidrug resistance protein 2 (MRP2; ABCC2) is an ATP-dependent export pump playing an important role in detoxification and chemoprotection. Human MRP2 is predominantly expressed at the apical membrane of hepatocytes, where it facilitates the elimination of a wide range of compounds, especially conjugates of lipophilic substances. In addition, MRP2 can transport uncharged compounds in cotransport with glutathione, and thus can modulate the pharmacokinetics of many drugs. The excretion of xenobiotic compounds decreases the efficiency of many drugs and a high MRP2 expression in cancer cells can be the reason for multidrug resistance.

Main localization:
Liver, kidney, small intestine (apical membranes)
Transporter assay:
Efflux transporter assay
Probe substrates:
5(6)-carboxy-2,'7'-dichlorofluorescein (CDCF)
Probe inhibitors:
MK-571, benzbromarone
Regulatory relevance:
Important interacting drugs:
Irinotecan, olmesartan, valsartan, vinblastin, benzbromarone, cyclosporine, indomethacin, ketoprofen, MK-571, probenecid, furosemide
From other species:

Inhibitory effect on hMRP2-mediated CDCF efflux by various drugs (100 µM)

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