Work

On the Intractability of Estrogen-Related Receptor α as a Target for Activation by Small Molecules

Year: 2007

Type: article

Abstract: 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.

Source: Journal of Medicinal Chemistry

DOI: 10.1021/jm7012387