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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

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journal contribution
posted on 05.05.2005, 00:00 by 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
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.