Skip to main content
Journal cover image

Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.

Publication ,  Journal Article
Zuercher, WJ; Gaillard, S; Orband-Miller, LA; Chao, EYH; Shearer, BG; Jones, DG; Miller, AB; Collins, JL; McDonnell, DP; Willson, TM
Published in: J Med Chem
May 5, 2005

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.

Duke Scholars

Altmetric Attention Stats
Dimensions Citation Stats

Published In

J Med Chem

DOI

ISSN

0022-2623

Publication Date

May 5, 2005

Volume

48

Issue

9

Start / End Page

3107 / 3109

Location

United States

Related Subject Headings

  • Transcription Factors
  • Structure-Activity Relationship
  • Receptors, Estrogen
  • Phenols
  • Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha
  • Molecular Mimicry
  • Medicinal & Biomolecular Chemistry
  • Ligands
  • Hydrazines
  • Humans
 

Citation

APA
Chicago
ICMJE
MLA
NLM
Zuercher, W. J., Gaillard, S., Orband-Miller, L. A., Chao, E. Y. H., Shearer, B. G., Jones, D. G., … Willson, T. M. (2005). Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma. J Med Chem, 48(9), 3107–3109. https://doi.org/10.1021/jm050161j
Zuercher, William J., Stéphanie Gaillard, Lisa A. Orband-Miller, Esther Y. H. Chao, Barry G. Shearer, David G. Jones, Aaron B. Miller, Jon L. Collins, Donald P. McDonnell, and Timothy M. Willson. “Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.J Med Chem 48, no. 9 (May 5, 2005): 3107–9. https://doi.org/10.1021/jm050161j.
Zuercher WJ, Gaillard S, Orband-Miller LA, Chao EYH, Shearer BG, Jones DG, et al. Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma. J Med Chem. 2005 May 5;48(9):3107–9.
Zuercher, William J., et al. “Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.J Med Chem, vol. 48, no. 9, May 2005, pp. 3107–09. Pubmed, doi:10.1021/jm050161j.
Zuercher WJ, Gaillard S, Orband-Miller LA, Chao EYH, Shearer BG, Jones DG, Miller AB, Collins JL, McDonnell DP, Willson TM. Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma. J Med Chem. 2005 May 5;48(9):3107–3109.
Journal cover image

Published In

J Med Chem

DOI

ISSN

0022-2623

Publication Date

May 5, 2005

Volume

48

Issue

9

Start / End Page

3107 / 3109

Location

United States

Related Subject Headings

  • Transcription Factors
  • Structure-Activity Relationship
  • Receptors, Estrogen
  • Phenols
  • Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha
  • Molecular Mimicry
  • Medicinal & Biomolecular Chemistry
  • Ligands
  • Hydrazines
  • Humans