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.

Full Text

Duke Authors

Cited Authors

  • Hyatt, SM; Lockamy, EL; Stein, RA; McDonnell, DP; Miller, AB; Orband-Miller, LA; Willson, TM; Zuercher, WJ

Published Date

  • December 27, 2007

Published In

Volume / Issue

  • 50 / 26

Start / End Page

  • 6722 - 6724

PubMed ID

  • 18052088

Pubmed Central ID

  • PMC2556064

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/jm7012387


  • eng

Conference Location

  • United States