Constitutive Androstane Receptor

Supporting information

The constitutive androstane receptor (CAR) is a member of the NR1I family of nuclear receptors, along with the pregnane X receptor and vitamin D receptor. CAR is involved in the sensing and clearance of foreign toxins through the upregulation of genes involved in xenobiotic clearance, including cytochrome P450, bilirubin, and multidrug transporters.

The name 'constitutive androstane receptor' refers to the unusual, constitutively active status of this receptor when not occupied by a ligand. Active constitutive androstane receptors bind to DNA as a heterodimer with RXRα, where they share common response elements with pregnane X receptors. The activity of these receptors is inhibited by the androstane metabolites, androstenol and androstanol, and can be induced by hypoxia inducible factor (HIF) activation. Recent research suggests that interactions between CAR and HIF lead to a reciprocal modulation of function.

In addition to its role in xenobiotic substance detection and clearance, the constitutive androstane receptor is also involved in the regulation of fatty acid β oxidation, gluconeogenesis and lipid metabolism. As a result, the constitutive androstane receptor is under investigation as a potential therapeutic target for metabolic disorders.

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Gene Species Gene Symbol Gene Accession No. Protein Accession No.
Constitutive Androstane Receptor Human NR1I3 NM_001077469 Q14994
Mouse Nr1i3 NM_009803 O35627
Rat Nr1i3 NM_001270838 Q9QUS1

Literature for Constitutive Androstane Receptor

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