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Bioorg Med Chem Lett. 2005 Mar 1;15(5):1311-3.

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

Author information

  • 1Department of Gene regulation and Drug Discovery, The Beckman Research Institute, The City of Hope National Medical Center, The Gonda Diabetes and Genetic Research Center, Duarte, CA 91010, USA.

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.

PMID:
15713377
[PubMed - indexed for MEDLINE]
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