蛋白质水解
化学
雌激素受体
诱导剂
降级(电信)
组合化学
雌激素
受体
药理学
计算生物学
生物化学
立体化学
计算机科学
生物
医学
内科学
酶
基因
电信
癌症
乳腺癌
作者
Lijie Peng,Zhensheng Zhang,Chong Lei,Shan Li,Zhang Zhang,Xiaomei Ren,Yu Chen,Yan Zhang,Yong Xu,Ke Ding
标识
DOI:10.1021/acsmedchemlett.9b00025
摘要
A series of (E)-3-(4-((2,4-bis(trifluoromethyl)benzyl)oxy)-3-methoxyphenyl)-2-cyanoacrylamide derivatives were designed and synthesized as new estrogen-related receptor α (ERRα) degraders based on the proteolysis targeting chimera (PROTAC) concept.One of the representative compounds 6c is capable of specifically degrading ERRα protein by >80% at a relatively low concentration of 30 nM, becoming one of the most potent and selective ERRα degraders to date.Compound 6c could be utilized as a new powerful research tool for further biological investigation of ERRα.
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