| Literature DB >> 16307879 |
Esther Y H Chao1, Jon L Collins, Stéphanie Gaillard, Aaron B Miller, Liping Wang, Lisa A Orband-Miller, Robert T Nolte, Donald P McDonnell, Timothy M Willson, William J Zuercher.
Abstract
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.Entities:
Mesh：
Substances：
Year: 2005 PMID： 16307879 DOI： 10.1016/j.bmcl.2005.11.030
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823