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ID: ALA1141994

Journal: Bioorg Med Chem Lett

Title: Identification of an agonist ligand for estrogen-related receptors ERRbeta/gamma.

Authors: Yu DD, Forman BM.

Abstract: In order to develop agonist ligands that are specific for the estrogen-related receptors ERRbeta/gamma, a hydrazone with a 4-hydroxy group at one phenyl ring and a 4-diethylamino moiety at the other phenyl ring was synthesized. We demonstrate that compound 3 (DY131; N'-{(1E)-[4-(diethylamino)phenyl]methylene}-4-hydroxybenzohydrazide) effectively and selectively activates ERRbeta/gamma. DY131 had no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta). This work defines a convenient synthesis for a novel and selective pharmacologic tool that can be used to elucidate the biological activities of ERRbeta/gamma.

CiteXplore: 15713377

DOI: 10.1016/j.bmcl.2005.01.025