Constitutive Androstane Receptor
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. The principal function of the constitutive androstane receptor is the sensing and clearance of foreign toxins.
Constitutive Androstane Receptor Agonists |
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|---|---|
| Cat. No. | Product Name / Activity |
| 3683 | CITCO |
| Selective CAR agonist | |
Constitutive Androstane Receptor Inverse Agonists |
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| Cat. No. | Product Name / Activity |
| 4096 | Clotrimazole |
| CAR inverse agonist; Also Cytochrome P450 inhibitor | |
| 2373 | T 0901317 |
| CAR inverse agonist; Also potent LXR agonist | |
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.