Molnár Ferdinand, Küblbeck Jenni, Jyrkkärinne Johanna, Prantner Viktória, Honkakoski Paavo
School of Pharmacy, Faculty of Health Sciences and Biocenter Kuopio, University of Eastern Finland, PO Box 1627, FI-70211 Kuopio, Finland.
Drug Metabol Drug Interact. 2013;28(2):79-93. doi: 10.1515/dmdi-2013-0009.
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.
组成型雄烷受体（CAR；NR1I3）已成为主要的药物和外源性物质敏感转录调节因子之一。它对多种氧化酶、结合酶和转运蛋白的表达有重大影响，因此，CAR可能导致药物/药物相互作用。CAR的新功能也不断涌现：它能够调节葡萄糖、脂质和胆汁酸的代谢命运，还参与细胞间通讯、细胞周期调控和化学致癌作用。在此，我们将综述关于CAR及其靶基因表达、与伴侣蛋白的相互作用和作用机制、个体间和种属差异，以及CAR配体选择性的最新信息和用于研究其配体的方法。
