Androstane metabolites bind to and deactivate the nuclear receptor CAR-β

@article{Forman1998AndrostaneMB,
  title={Androstane metabolites bind to and deactivate the nuclear receptor CAR-β},
  author={B. M. Forman and I. Tzameli and Hueng-Sik Choi and Jasmine Chen and D. Simha and W. Seol and R. Evans and D. Moore},
  journal={Nature},
  year={1998},
  volume={395},
  pages={612-615}
}
The orphan receptor CAR-β (ref. 1) binds DNA as a heterodimer with the retinoid-X receptor and activates gene transcription in a constitutive manner. Here we show that, in contrast to the classical nuclear receptors, the constitutive activity of CAR-β results from a ligand-independent recruitment of transcriptional co-activators. While searching for potential ligands of CAR-β, we found that the steroids androstanol and androstenol inhibit the constitutive activity of CAR-β. This effect is… Expand
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