Ontology highlight
ABSTRACT:
SUBMITTER: Peng L
PROVIDER: S-EPMC6512006 | biostudies-literature | 2019 May
REPOSITORIES: biostudies-literature
Peng Lijie L Zhang Zhensheng Z Lei Chong C Li Shan S Zhang Zhang Z Ren Xiaomei X Chang Yu Y Zhang Yan Y Xu Yong Y Ding Ke K
ACS medicinal chemistry letters 20190412 5
A series of (<i>E</i>)-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 <b>6c</b> 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 <b>6c</b> could b ...[more]