CAR PXR
RXR and its Brothers

Author: Gianpiero Pescarmona
Date: 17/07/2011

Description

DEFINITION

The constitutive androstane receptor - CAR also known as nuclear receptor subfamily 1, group I, member 3 is a protein that in humans is encoded by the NR1I3 gene. CAR is a member of the nuclear receptor superfamily and along with Pregnane X receptor - 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. Hence CAR (and PXR) are important in the detoxification of foreign substances such as drugs.

THE GENE

DatabaseLink
WikigenesACADM
GeneCards"URL":
Your Favorite Gene Sigma"URL":

Wikigenes includes links to

  • NCBI Gene
  • NCBI SNP
  • iHOP resource
  • OMIM
  • SNPedia
  • UniProt
  • Ensembl
  • HGNC

CHEMICAL STRUCTURE AND IMAGES

When relevant for the function

  • Primary structure
  • Secondary structure
  • Tertiary structure
  • Quaternary structure


Protein Aminoacids Percentage
The Protein Aminoacids Percentage gives useful information on the local environment and the metabolic status of the cell (starvation, lack of essential AA, hypoxia)

Protein Aminoacids Percentage (Width 700 px)

SYNTHESIS AND TURNOVER

mRNA synthesis
protein synthesis

post-translational modifications
degradation

CELLULAR FUNCTIONS

cellular localization,
biological function

CAR is a member of the nuclear receptor superfamily, and is a key regulator of xenobiotic and endobiotic metabolism. The protein binds to DNA as a monomer or a heterodimer with RXR 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,
  • steroid hormones
  • prescription drugs
  • a variety of environmental foreign compounds
DatabaseLink
KEGG Pathways"URL":
Human Metabolome Database"URL":
  • Cell signaling and Ligand transport

REGULATION

DIAGNOSTIC USE

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