An update on the constitutive androstane receptor (CAR)

Drug Metabol Drug Interact. 2013;28(2):79-93. doi: 10.1515/dmdi-2013-0009.


The constitutive androstane receptor (CAR; NR1I3) has emerged as one of the main drug- and xenobiotic-sensitive transcriptional regulators. It has a major effect on the expression of several oxidative and conjugative enzymes and transporters, and hence, CAR can contribute to drug/drug interactions. Novel functions for CAR are also emerging: it is able to modulate the metabolic fate of glucose, lipids, and bile acids, and it is also involved in cell-cell communication, regulation of the cell cycle, and chemical carcinogenesis. Here, we will review the recent information available on CAR and its target gene expression, its interactions with partner proteins and mechanisms of action, interindividual and species variation, and current advances in CAR ligand selectivity and methods used in interrogation of its ligands.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Biological Evolution
  • Constitutive Androstane Receptor
  • DNA / metabolism
  • Humans
  • Ligands
  • Models, Molecular
  • Receptors, Cytoplasmic and Nuclear / chemistry
  • Receptors, Cytoplasmic and Nuclear / physiology*
  • Species Specificity


  • Constitutive Androstane Receptor
  • Ligands
  • NR1I3 protein, human
  • Receptors, Cytoplasmic and Nuclear
  • DNA