Part:BBa_K364306:Experience

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Ligand

Unlike most nuclear receptors, CAR 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.

Physiological effects

Along with PXR functions as a sensor of endobiotic and xenobiotic substances and in response upregulates the expression of proteins responsible for the metabolism and excretion of these substances. 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.

Applications of BBa_K364306

This part can be fused with different DBDs in order to make a Nuclear hormone receptor for different applications, such as for measuring endobiotic and xenobiotic substances.

References

Baes M, Gulick T, Choi HS, Martinoli MG, Simha D, Moore DD (March 1994). "A new orphan member of the nuclear hormone receptor superfamily that interacts with a subset of retinoic acid response elements". Mol. Cell. Biol. 14 (3): 1544–52.

Wada T, Gao J, Xie W (August 2009). "PXR and CAR in energy metabolism". Trends Endocrinol. Metab. 20 (6): 273–9.

Choi HS, Chung M, Tzameli I, et al. (1997). "Differential transactivation by two isoforms of the orphan nuclear hormone receptor CAR.". J. Biol. Chem. 272 (38): 23565–71.

Forman BM, Tzameli I, Choi HS, et al. (1998). "Androstane metabolites bind to and deactivate the nuclear receptor CAR-beta.". Nature 395 (6702): 612–5.

Chang TK, Bandiera SM, Chen J (2003). "Constitutive androstane receptor and pregnane X receptor gene expression in human liver: interindividual variability and correlation with CYP2B6 mRNA levels.". Drug Metab. Dispos. 31 (1): 7–10.

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