Role reversal: new insights from new ligands for the xenobiotic receptor CAR.
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.
Tzameli
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Beth Israel Deaconness Medical Center, Dept of Medicine, Division of Endocrinology and Metabolism, 99 Brookline Avenue, Boston, MA 0221, USA.
Moore
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D000818:Animals; D000090702:Constitutive Androstane Receptor; D006801:Humans; D008024:Ligands; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists / Q000187:drug effects / Q000502:physiology*; D015398:Signal Transduction / Q000502:physiology; D014157:Transcription Factors / Q000819:agonists / Q000187:drug effects / Q000502:physiology*
D000090702:Constitutive Androstane Receptor; D008024:Ligands; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors