
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.
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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
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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.

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