Identification and Structure-activity Relationship of Phenolic Acyl Hydrazones As Selective Agonists for the Estrogen-related Orphan Nuclear Receptors ERRbeta and ERRgamma

Overview

Journal J Med Chem

Publisher American Chemical Society

Specialty Chemistry

Date 2005 Apr 29

PMID 15857113

Citations 41

Authors

William J Zuercher

Stephanie Gaillard

Lisa A Orband-Miller

Esther Y H Chao

Barry G Shearer

David G Jones

Aaron B Miller

Jon L Collins

Donald P McDonnell

Timothy M Willson

Affiliations

Soon will be listed here.

Abstract

The first small molecule agonists of the estrogen-related receptors have been identified. GSK4716 (3) and GSK9089 (4) show binding to ERRgamma with remarkable selectivity over the classical estrogen receptors. Notably, in cell-based reporter assays, 3 mimics the protein ligand PGC-1alpha in activation of human ERRbeta and ERRgamma.

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