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

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

  • J Med Chem. 2004 Nov 4;47(23):5593-6. doi: 10.1021/jm049334f.
Brett B Busch 1,  William C Stevens Jr,  Richard Martin,  Peter Ordentlich,  Sihong Zhou,  Douglas W Sapp,  Robert A Horlick,  Raju Mohan
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, X-Ceptor Therapeutics, Inc., 4757 Nexus Center Drive, San Diego, California 92121, USA.
PMID: 15509154 DOI: 10.1021/jm049334f
Abstract

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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