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ID: ALA1137227

Journal: J Med Chem

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

Authors: Busch BB, Stevens WC, Martin R, Ordentlich P, Zhou S, Sapp DW, Horlick RA, Mohan R.

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.

CiteXplore: 15509154

DOI: 10.1021/jm049334f