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Identification and Structure−Activity Relationship of Phenolic Acyl Hydrazones as Selective Agonists for the Estrogen-Related Orphan Nuclear Receptors ERRβ and ERRγ

Year: 2005
Type: article
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.
DOI: 10.1021/jm050161j
Authors: 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
Institution: Duke University
Language: English
Subfield: Genetics
Open Access status: green
OpenAlex ID: W2015985353
FWCI: 3.193
Cites: 11
Cited by: 103
Related to: 10