Identification and Structure−ActivityRelationship of Phenolic AcylHydrazones as Selective Agonists for theEstrogen-Related Orphan NuclearReceptors ERRβ and ERRγ
The first small molecule agonists of the estrogen-related receptors have been identified. GSK4716 (3) andGSK9089 (4) show binding to ERRγ with remarkable selectivity over the classical estrogen receptors. Notably, in cell-basedreporter assays, 3 mimics the protein ligand PGC-1α inactivation of human ERRβ and ERRγ.