On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.
Publication
, Journal Article
Hyatt, SM; Lockamy, EL; Stein, RA; McDonnell, DP; Miller, AB; Orband-Miller, LA; Willson, TM; Zuercher, WJ
Published in: J Med Chem
December 27, 2007
The estrogen-related receptor alpha (ERRalpha) is a potential target for activation in the treatment of metabolic disease. To date, no small-molecule agonists of ERRalpha have been identified despite several high-throughput screening campaigns. We describe the synthesis and profiling of a small array of compounds designed on the basis of a previously reported agonist-bound crystal structure of the closely related receptor ERRgamma. The results suggest that ERRalpha may be intractable as a direct target for pharmacologic activation.
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Published In
J Med Chem
DOI
ISSN
0022-2623
Publication Date
December 27, 2007
Volume
50
Issue
26
Start / End Page
6722 / 6724
Location
United States
Related Subject Headings
- Receptors, Estrogen
- Medicinal & Biomolecular Chemistry
- Hydrazones
- Humans
- Hela Cells
- HeLa Cells
- Fluorescence Resonance Energy Transfer
- ERRalpha Estrogen-Related Receptor
- Drug Inverse Agonism
- Crystallography, X-Ray
Citation
APA
Chicago
ICMJE
MLA
NLM
Hyatt, S. M., Lockamy, E. L., Stein, R. A., McDonnell, D. P., Miller, A. B., Orband-Miller, L. A., … Zuercher, W. J. (2007). On the intractability of estrogen-related receptor alpha as a target for activation by small molecules. J Med Chem, 50(26), 6722–6724. https://doi.org/10.1021/jm7012387
Hyatt, Stephen M., Elizabeth L. Lockamy, Rebecca A. Stein, Donald P. McDonnell, Aaron B. Miller, Lisa A. Orband-Miller, Timothy M. Willson, and William J. Zuercher. “On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.” J Med Chem 50, no. 26 (December 27, 2007): 6722–24. https://doi.org/10.1021/jm7012387.
Hyatt SM, Lockamy EL, Stein RA, McDonnell DP, Miller AB, Orband-Miller LA, et al. On the intractability of estrogen-related receptor alpha as a target for activation by small molecules. J Med Chem. 2007 Dec 27;50(26):6722–4.
Hyatt, Stephen M., et al. “On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.” J Med Chem, vol. 50, no. 26, Dec. 2007, pp. 6722–24. Pubmed, doi:10.1021/jm7012387.
Hyatt SM, Lockamy EL, Stein RA, McDonnell DP, Miller AB, Orband-Miller LA, Willson TM, Zuercher WJ. On the intractability of estrogen-related receptor alpha as a target for activation by small molecules. J Med Chem. 2007 Dec 27;50(26):6722–6724.
Published In
J Med Chem
DOI
ISSN
0022-2623
Publication Date
December 27, 2007
Volume
50
Issue
26
Start / End Page
6722 / 6724
Location
United States
Related Subject Headings
- Receptors, Estrogen
- Medicinal & Biomolecular Chemistry
- Hydrazones
- Humans
- Hela Cells
- HeLa Cells
- Fluorescence Resonance Energy Transfer
- ERRalpha Estrogen-Related Receptor
- Drug Inverse Agonism
- Crystallography, X-Ray