Constitutive androstane receptor

NR1I3
Available structures
PDBOrtholog search: PDBe RCSB
Identifiers
AliasesNR1I3, CAR, CAR1, MB67, nuclear receptor subfamily 1 group I member 3
External IDsOMIM: 603881; MGI: 1346307; HomoloGene: 3759; GeneCards: NR1I3; OMA:NR1I3 - orthologs
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_001243062
NM_001243063
NM_009803

RefSeq (protein)

NP_001229991
NP_001229992
NP_033933

Location (UCSC)Chr 1: 161.23 – 161.24 MbChr 1: 171.04 – 171.05 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

The constitutive androstane receptor (CAR) also known as nuclear receptor subfamily 1, group I, member 3 is a protein that in humans is encoded by the NR1I3 gene.[5] CAR is a member of the nuclear receptor superfamily and along with pregnane X receptor (PXR) functions as a sensor of endobiotic and xenobiotic substances. In response, expression of proteins responsible for the metabolism and excretion of these substances is upregulated.[6] Hence, CAR and PXR play a major role in the detoxification of foreign substances such as drugs.

Androstenol and several isomers of androstanol, androstanes, are endogenous antagonists of the CAR, and despite acting as antagonists, were the basis for the naming of this receptor.[7] More recently, dehydroepiandrosterone (DHEA), also an androstane, has been found to be an endogenous agonist of the CAR.[8]

  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000143257Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000005677Ensembl, May 2017
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ Baes M, Gulick T, Choi HS, Martinoli MG, Simha D, Moore DD (Mar 1994). "A new orphan member of the nuclear hormone receptor superfamily that interacts with a subset of retinoic acid response elements". Molecular and Cellular Biology. 14 (3): 1544–52. doi:10.1128/mcb.14.3.1544. PMC 358513. PMID 8114692.
  6. ^ Wada T, Gao J, Xie W (Aug 2009). "PXR and CAR in energy metabolism". Trends in Endocrinology and Metabolism. 20 (6): 273–9. doi:10.1016/j.tem.2009.03.003. PMID 19595610. S2CID 25764831.
  7. ^ Nicholas A. Meanwell (8 December 2014). Tactics in Contemporary Drug Design. Springer. pp. 182–. ISBN 978-3-642-55041-6.
  8. ^ Kohalmy K, Tamási V, Kóbori L, Sárváry E, Pascussi JM, Porrogi P, et al. (2007). "Dehydroepiandrosterone induces human CYP2B6 through the constitutive androstane receptor". Drug Metab. Dispos. 35 (9): 1495–501. doi:10.1124/dmd.107.016303. PMC 2423426. PMID 17591676.