On the intractability of estrogen-related receptor α as a target for activation by small molecules

…, AB Miller, LA Orband-Miller, TM Willson…

文献索引：Hyatt, Stephen M.; Lockamy, Elizabeth L.; Stein, Rebecca A.; McDonnell, Donald P.; Miller, Aaron B.; Orband-Miller, Lisa A.; Willson, Timothy M.; Zuercher, William J. Journal of Medicinal Chemistry, 2007 , vol. 50, # 26 p. 6722 - 6724

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被引用次数: 19

摘要

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 ...