Portal de Periódicos da CAPES

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

2005; American Chemical Society; Volume: 48; Issue: 9 Linguagem: Inglês

10.1021/jm050161j

1520-4804

William J. Zuercher, Stéphanie Gaillard, Lisa A. Orband‐Miller, Esther Y. Chao, Barry G. Shearer, David G. Jones, Aaron B. Miller, Jon L. Collins, Donald P. McDonnell, Timothy M. Willson,

Organic Chemistry Cycloaddition Reactions

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.