Role reversal: new insights from new ligands for the xenobiotic receptor CAR

Trends Endocrinol Metab. 2001 Jan-Feb;12(1):7-10. doi: 10.1016/s1043-2760(00)00332-5.


In the classic model of nuclear receptor signaling, specific hormone binding results in the recruitment of coactivator proteins and transcriptional activation. Recent results with newly characterized nuclear receptors have expanded this model to include new types of ligands and novel transcriptional responses. Both inverse agonists and conventional agonist ligands have been identified for the xenobiotic receptor constitutive androstane receptor (CAR), a constitutive activator of transcription in the absence of ligands.

Publication types

  • Review

MeSH terms

  • Animals
  • Constitutive Androstane Receptor
  • Humans
  • Ligands
  • Receptors, Cytoplasmic and Nuclear / agonists
  • Receptors, Cytoplasmic and Nuclear / drug effects
  • Receptors, Cytoplasmic and Nuclear / physiology*
  • Signal Transduction / physiology
  • Transcription Factors / agonists
  • Transcription Factors / drug effects
  • Transcription Factors / physiology*


  • Constitutive Androstane Receptor
  • Ligands
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors