Constitutive Androstane Receptor (CAR)

Constitutive Androstane Receptor Overview

The Constitutive Androstane Receptor (CAR), encoded by the NR1I3 gene, is a nuclear receptor that functions as a sensor for both endogenous substances (endobiotics) and foreign compounds (xenobiotics). It is constitutively active and regulates the transcription of genes involved in drug metabolism, glucose homeostasis, lipid metabolism, and other physiological processes. CAR is primarily expressed in the liver but also found in the kidneys, intestines, and stomach. Its activation, either directly by ligands or indirectly via signaling pathways, leads to its translocation to the nucleus where it modulates gene expression, impacting drug disposition, toxicity, and metabolic regulation. CAR is implicated in diseases such as diabetes, fatty liver disease, and cancer, making it a potential therapeutic target.

Mechanism of Action

Agonist or inverse agonist binding regulates transcription of target genes involved in drug metabolism, glucose homeostasis, lipid metabolism and other pathways.

Biological Functions

Safety Considerations

Interacting Drugs

Associated Biomarkers