Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.

Journal Article (Journal Article)

The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared with that of 4-OHT. An X-ray crystal structure of one of the designed compounds bound to ERRgamma LBD confirms the molecular basis of the selectivity.

Full Text

Duke Authors

Cited Authors

  • Chao, EYH; Collins, JL; Gaillard, S; Miller, AB; Wang, L; Orband-Miller, LA; Nolte, RT; McDonnell, DP; Willson, TM; Zuercher, WJ

Published Date

  • February 15, 2006

Published In

Volume / Issue

  • 16 / 4

Start / End Page

  • 821 - 824

PubMed ID

  • 16307879

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2005.11.030

Language

  • eng

Conference Location

  • England