An update on the constitutive androstane receptor (CAR).

Ferdinand Molnár, Jenni Küblbeck, Johanna Jyrkkärinne, Viktória Prantner, Paavo Honkakoski

School of Pharmacy, Faculty of Health Sciences and Biocenter Kuopio, University of Eastern Finland, PO Box 1627, FI-70211 Kuopio, Finland. paavo.honkakoski@uef.fi

Drug metabolism and drug interactions 2013

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The constitutive androstane receptor (CAR; NR1I3) has emerged as one of the main drug- and xenobiotic-sensitive transcriptional regulators. It has a major effect on the expression of several oxidative and conjugative enzymes and transporters, and hence, CAR can contribute to drug/drug interactions. Novel functions for CAR are also emerging: it is able to modulate the metabolic fate of glucose, lipids, and bile acids, and it is also involved in cell-cell communication, regulation of the cell cycle, and chemical carcinogenesis. Here, we will review the recent information available on CAR and its target gene expression, its interactions with partner proteins and mechanisms of action, interindividual and species variation, and current advances in CAR ligand selectivity and methods used in interrogation of its ligands.

Citation

Ferdinand Molnár, Jenni Küblbeck, Johanna Jyrkkärinne, Viktória Prantner, Paavo Honkakoski. An update on the constitutive androstane receptor (CAR). Drug metabolism and drug interactions. 2013;28(2):79-93