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
Pubmed Central 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