Constitutive Androstane Receptor (CAR)

NR1I3; NR1-I3; CAR1; MB67; Nuclear Receptor Subfamily 1,Group I,Member 3; Constitutive active response; Constitutive activator of retinoid response; Orphan nuclear receptor MB67

SPN	U426
HGNC	7969
MGI	1346307
PubMed	22098234
RGD	621400
UniProt	Q14994
Wiki	CAR

CAR is a member of the nuclear receptor superfamily, and is a key regulator of xenobiotic and endobiotic metabolism. The protein binds to DNA as a monomer or a heterodimer with the retinoid X receptor and regulates the transcription of target genes involved in drug metabolism and bilirubin clearance, such as cytochrome P450 family members. Unlike most nuclear receptors, this transcriptional regulator is constitutively active in the absence of ligand but is regulated by both agonists and inverse agonists. Ligand binding results in translocation of this protein to the nucleus, where it activates or represses target gene transcription. These ligands include bilirubin, a variety of foreign compounds, steroid hormones, and prescription drugs. Multiple transcript variants encoding different isoforms have been found for this gene.

Reference

"A new orphan member of the nuclear hormone receptor superfamily that interacts with a subset of retinoic acid response elements."
Mol. Cell. Biol. 14:1544-1552(1994) [PubMed] [Europe PMC] [Abstract]

"Expression of constitutive androstane receptor splice variants in human tissues and their functional consequences."
J. Pharmacol. Exp. Ther. 311:811-821(2004) [PubMed] [Europe PMC] [Abstract]

"The DNA sequence and biological annotation of human chromosome 1."
Nature 441:315-321(2006) [PubMed] [Europe PMC] [Abstract]

"The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)."
Genome Res. 14:2121-2127(2004) [PubMed] [Europe PMC] [Abstract]

"A component of the 26S proteasome binds on orphan member of the nuclear hormone receptor superfamily."
J. Steroid Biochem. Mol. Biol. 56:23-30(1996) [PubMed] [Europe PMC] [Abstract]

"Cytoplasmic accumulation of the nuclear receptor CAR by a tetratricopeptide repeat protein in HepG2 cells."
Mol. Pharmacol. 64:1069-1075(2003) [PubMed] [Europe PMC] [Abstract]

"Dephosphorylation of threonine 38 is required for nuclear translocation and activation of human xenobiotic receptor CAR (NR1I3)."
J. Biol. Chem. 284:34785-34792(2009) [PubMed] [Europe PMC] [Abstract]

"A structural basis for constitutive activity in the human CAR/RXRalpha heterodimer."
Mol. Cell 16:919-928(2004) [PubMed] [Europe PMC] [Abstract]

"Twenty-six novel single nucleotide polymorphisms and their frequencies of the NR1I3 (CAR) gene in a Japanese population."
Drug Metab. Pharmacokinet. 18:413-418(2003) [PubMed] [Europe PMC] [Abstract]