2. Academic Validation
  3. Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma

Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma

  • J Med Chem. 2005 May 5;48(9):3107-9. doi: 10.1021/jm050161j.
William J Zuercher 1,  Stéphanie Gaillard,  Lisa A Orband-Miller,  Esther Y H Chao,  Barry G Shearer,  David G Jones,  Aaron B Miller,  Jon L Collins,  Donald P McDonnell,  Timothy M Willson
Affiliations

Affiliation

  • 1 Discovery Research, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, North Carolina 27707, USA. [email protected]
PMID: 15857113 DOI: 10.1021/jm050161j
Abstract

The first small molecule agonists of the estrogen-related receptors have been identified. GSK4716 (3) and GSK9089 (4) show binding to ERRgamma with remarkable selectivity over the classical estrogen receptors. Notably, in cell-based reporter assays, 3 mimics the protein ligand PGC-1alpha in activation of human ERRbeta and ERRgamma.

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