Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 16, Issue 4, Pages 821-824Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.11.030
Keywords
ERR gamma; chemical tool; orphan nuclear receptor
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Funding
- NIDDK NIH HHS [U19 DK062434] Funding Source: Medline
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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 ERR gamma LBD confirms the molecular basis of the selectivity. (c) 2005 Elsevier Ltd. All rights reserved.
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