2. Academic Validation
  3. Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation

Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation

  • ACS Med Chem Lett. 2019 Apr 12;10(5):767-772. doi: 10.1021/acsmedchemlett.9b00025.
Lijie Peng 1,  Zhensheng Zhang 1,  Chong Lei 1,  Shan Li 1,  Zhang Zhang 1,  Xiaomei Ren 1,  Yu Chang 1,  Yan Zhang 2,  Yong Xu 2,  Ke Ding 1
Affiliations

Affiliations

  • 1 International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development, Ministry of Education (MOE) of China, Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China.
  • 2 Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, 190 Kaiyuan Avenue, Guangzhou 510530, China.
PMID: 31097997 DOI: 10.1021/acsmedchemlett.9b00025
Abstract

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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