基于结构导向合成对孤儿雌激素相关受体γ（ERRγ）具有更高选择性的他莫昔芬类似物。
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
作者信息
Chao Esther Y H, Collins Jon L, Gaillard Stéphanie, Miller Aaron B, Wang Liping, Orband-Miller Lisa A, Nolte Robert T, McDonnell Donald P, Willson Timothy M, Zuercher William J
机构信息
Discovery Research, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA.
出版信息
Bioorg Med Chem Lett. 2006 Feb 15;16(4):821-4. doi: 10.1016/j.bmcl.2005.11.030. Epub 2005 Nov 22.
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.
本文描述了4-羟基他莫昔芬（4-OHT）衍生物的设计与合成。这些化合物对孤儿雌激素相关受体γ和经典雌激素受体α的结合亲和力表明，与4-OHT相比，带有羟烷基的类似物显示出更好的结合选择性。一种设计化合物与ERRγ配体结合域（LBD）的X射线晶体结构证实了这种选择性的分子基础。
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