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Identification of New Small-Molecule Inducers of Estrogen-related Receptor ? (ERR?) Degradation.

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 ? (ERR?) degraders based on the proteolysis targeting chimera (PROTAC) concept. One of the representative compounds 6c is capable of specifically degrading ERR? protein by >80% at a relatively low concentration of 30 nM, becoming one of the most potent and selective ERR? degraders to date. Compound 6c could be utilized as a new powerful research tool for further biological investigation of ERR?.

SUBMITTER: Peng L 

PROVIDER: S-EPMC6512006 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature

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

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]

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