On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.
Journal Article (Journal Article)
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.
- Hyatt, SM; Lockamy, EL; Stein, RA; McDonnell, DP; Miller, AB; Orband-Miller, LA; Willson, TM; Zuercher, WJ
- December 27, 2007
Volume / Issue
- 50 / 26
Start / End Page
- 6722 - 6724
Pubmed Central ID
International Standard Serial Number (ISSN)
Digital Object Identifier (DOI)
- United States