CAR: detailing new models.
Functional analysis has broadened our understanding of the physiological roles of the two related nuclear receptors pregnane X receptor (PXR; NR1I2) and constitutive androstane receptor (CAR; NR1I3). Initial research focused on the role of these two receptors in xenobiotic detoxification and, more recently, additional functional roles for CAR have been identified. Specifically, CAR activity has been shown to ameliorate the effects of hyperbilirubinemia, caloric restriction and toxic bile acids. Thus, the physiological role of CAR has broadened to include responses to metabolic and nutritional stress. These data highlight potential new opportunities in targeting CAR for drug discovery.
Goodwin
Bryan
B
High Throughput Biology, Discovery Research, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
Moore
John T
JT
D000818:Animals; D002779:Cholestasis / Q000188:drug therapy / Q000378:metabolism; D000090702:Constitutive Androstane Receptor; D006801:Humans; D006932:Hyperbilirubinemia / Q000188:drug therapy / Q000378:metabolism; D009765:Obesity / Q000188:drug therapy / Q000378:metabolism; D000077297:Pregnane X Receptor; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists / Q000502:physiology*; D011987:Receptors, Steroid / Q000502:physiology; D014157:Transcription Factors / Q000819:agonists / Q000502:physiology*
D000090702:Constitutive Androstane Receptor; C000625852:NR1I2 protein, human; C000716327:NR1I3 protein, human; D000077297:Pregnane X Receptor; D018160:Receptors, Cytoplasmic and Nuclear; D011987:Receptors, Steroid; D014157:Transcription Factors