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

William J. Zuercher, 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

Research output: Contribution to journalArticlepeer-review

Abstract

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

Original languageEnglish (US)
Pages (from-to)3107-3109
Number of pages3
JournalJournal of medicinal chemistry
Volume48
Issue number9
DOIs
StatePublished - May 5 2005
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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