Regulation of Multidrug Resistance-associated Protein 2 (ABCC2) by the Nuclear Receptors Pregnane X Receptor, Farnesoid X-activated Receptor, and Constitutive Androstane Receptor

Kast-Woelbern, Heidi R.; Goodwin, Bryan; Tarr, Paul T.; Jones, Stacey A.; Anisfeld, Andrew M.; Stoltz, Catherine M.; Tontonoz, Peter; Kliewer, S. A.; Willson, Timothy M.; Edwards, Peter A.

doi:10.1074/jbc.m109326200

articleJournal of Biological ChemistryJan 1, 2002HYBRID OA

Regulation of Multidrug Resistance-associated Protein 2 (ABCC2) by the Nuclear Receptors Pregnane X Receptor, Farnesoid X-activated Receptor, and Constitutive Androstane Receptor

HRHeidi R. Kast-Woelbern BGBryan Goodwin PTPaul T. Tarr SAStacey A. Jones AMAndrew M. Anisfeld

Howard Hughes Medical Institute · GlaxoSmithKline (Netherlands) · +3 more institutions

PubMed

Indexed incrossrefdoajpubmed

Abstract

The multidrug resistance-associated protein 2 (MRP2, ABCC2), mediates the efflux of several conjugated compounds across the apical membrane of the hepatocyte into the bile canaliculi. We identified MRP2 in a screen designed to isolate genes that are regulated by the farnesoid X-activated receptor (FXR, NR1H4). MRP2 mRNA levels were induced following treatment of human or rat hepatocytes with either naturally occurring (chenodeoxycholic acid) or synthetic (GW4064) FXR ligands. In addition, we have shown that MRP2 expression is regulated by the pregnane X receptor (PXR, NR1I2) and constitutive androstane receptor (CAR, NR1I3). Thus, treatment of rodent hepatocytes with PXR or CAR agonists results in a robust…

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Topics & keywords

Topics

Keywords

Pregnane X receptor
Constitutive androstane receptor
Farnesoid X receptor
Multidrug resistance-associated protein 2
Nuclear receptor
Retinoid X receptor
Biology
Chemistry

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