2. Academic Validation
  3. Identification of an agonist ligand for estrogen-related receptors ERRbeta/gamma

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

  • Bioorg Med Chem Lett. 2005 Mar 1;15(5):1311-3. doi: 10.1016/j.bmcl.2005.01.025.
Donna D Yu 1,  Barry Marc Forman
Affiliations

Affiliation

  • 1 Department 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.
PMID: 15713377 DOI: 10.1016/j.bmcl.2005.01.025
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.

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