Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation
journal contributionposted on 12.04.2019 by Lijie Peng, Zhensheng Zhang, Chong Lei, Shan Li, Zhang Zhang, Xiaomei Ren, Yu Chang, Yan Zhang, Yong Xu, Ke Ding
Any type of content formally published in an academic journal, usually following a peer-review process.
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.