Constitutive androstane receptor

Constitutive androstane receptor (CAR) is a member of the nuclear receptor family of intracellular transcription factors. It is primarily known for its role in the regulation of xenobiotic metabolism and the body's response to foreign substances.

Function

CAR is a key regulator of xenobiotic-induced transcription of phase I (cytochrome P450s), phase II (conjugation) and phase III (transporter) genes in the liver. It is activated by a variety of endogenous and exogenous chemicals, including many drugs and environmental pollutants. Once activated, CAR translocates to the nucleus, where it binds to specific DNA sequences and regulates the transcription of target genes.

Structure

CAR is a protein that is encoded by the NR1I3 gene in humans. It consists of several domains, including a DNA-binding domain and a ligand-binding domain. The DNA-binding domain allows CAR to bind to specific DNA sequences, while the ligand-binding domain allows it to interact with various ligands.

Clinical significance

CAR plays a crucial role in drug metabolism and detoxification. It is involved in the metabolism of many drugs, including phenobarbital, rifampicin, and carbamazepine. Alterations in CAR function can affect drug efficacy and toxicity. In addition, CAR is implicated in several diseases, including diabetes, obesity, and cancer.

Research

Research on CAR has focused on its role in drug metabolism and disease. Studies have shown that CAR activation can induce drug metabolism and detoxification, protect against chemical-induced liver injury, and regulate energy homeostasis. In addition, CAR has been implicated in the development and progression of several types of cancer, including liver and lung cancer.

See also

• Nuclear receptor
• Xenobiotic metabolism
• Drug metabolism

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