Target intelligence / Profile preview

Constitutive Androstane Receptor (CAR)

Target
CAR
Molecular classification
Nuclear Receptor, Nuclear hormone receptor, Nuclear xenosensor receptor, Transcription factor
01

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.

Other names
NR1I3
02

Mechanism of action

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

03

Biological functions

Xenobiotic sensingEndobiotic sensingTranscriptional regulationDrug metabolismGlucose homeostasis regulationLipid metabolism regulationBile acid synthesis regulationCell proliferationTissue regeneration
04

Disease associations

Drug toxicityMetabolic diseasesDiabetesFatty liver diseaseCancer
05

Safety considerations

Drug interactions due to altered drug metabolismPotential species-specific responsesSide effects due to broad physiological roles
06

Interacting drugs

Dehydroepiandrosterone (DHEA)

6 more in the full profile.

07

Biomarkers

CAR activity as biomarker of toxicityCAR activity as biomarker of drug interactions

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