Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha.

@article{Busch2004IdentificationOA,
  title={Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha.},
  author={Brett B Busch and William Stevens and Richard Tyler Martin and Peter Ordentlich and Sihong Zhou and Douglas W. Sapp and Robert A. Horlick and Raju Mohan},
  journal={Journal of medicinal chemistry},
  year={2004},
  volume={47 23},
  pages={5593-6}
}
The estrogen-related receptor alpha (ERRalpha) is an orphan receptor belonging to the nuclear receptor superfamily. The physiological role of ERRalpha has yet to be established primarily because of lack of a natural ligand. Herein, we describe the discovery of the first potent and selective inverse agonist of ERRalpha. Through in vitro and in vivo studies, these ligands will elucidate the endocrine signaling pathways mediated by ERRalpha including association with human disease states. 

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