On the Intractability of Estrogen-Related Receptor α as a Target for Activation by Small Molecules
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- 作者：Stephen M. Hyatt ; Elizabeth L. Lockamy ; Rebecca A. Stein ; Donald P. McDonnell ; Aaron B. Miller ; Lisa A. Orband-Miller ; Timothy M. Willson ; William J. Zuercher
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：December 27, 2007
- 年：2007
- 卷：50
- 期：26
- 页码：6722 - 6724
- 全文大小：270K
- 年卷期：v.50,no.26(December 27, 2007)
- ISSN：1520-4804
文摘
The estrogen-related receptor α (ERRα) is a potential target for activation in the treatment of metabolic disease. To date, no small-molecule agonists of ERRα 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 ERRγ. The results suggest that ERRα may be intractable as a direct target for pharmacologic activation.