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

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • Zuercher, WJ; Gaillard, S; Orband-Miller, LA; Chao, EYH; Shearer, BG; Jones, DG; Miller, AB; Collins, JL; McDonnell, DP; Willson, TM

Published Date

  • May 5, 2005

Published In

Volume / Issue

  • 48 / 9

Start / End Page

  • 3107 - 3109

PubMed ID

  • 15857113

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/jm050161j

Language

  • eng

Conference Location

  • United States