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Design, Synthesis, and Biological Evaluation of MEK PROTACs.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2019-12-20 , DOI: 10.1021/acs.jmedchem.9b00810 Stefan Vollmer , Danen Cunoosamy , Huafei Lv 1 , Huanxi Feng 1 , Xia Li 1 , Ziyang Nan 1 , Wenzhen Yang 1 , Matthew W D Perry
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2019-12-20 , DOI: 10.1021/acs.jmedchem.9b00810 Stefan Vollmer , Danen Cunoosamy , Huafei Lv 1 , Huanxi Feng 1 , Xia Li 1 , Ziyang Nan 1 , Wenzhen Yang 1 , Matthew W D Perry
Affiliation
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PROteolysis TArgeting Chimeras (PROTACs) targeting the degradation of MEK have been designed based on allosteric MEK inhibitors. Inhibition of the phosphorylation of ERK1/2 was less effective with the PROTACs than a small-molecule inhibitor; the best PROTACs, however, were more effective in inhibiting proliferation of A375 cells than an inhibitor.
中文翻译：
MEK PROTAC的设计，合成和生物学评估。
已经基于变构MEK抑制剂设计了针对MEK降解的蛋白水解靶嵌合体（PROTAC）。用PROTAC抑制ERK1 / 2磷酸化的效果不如使用小分子抑制剂。然而，最好的PROTACs在抑制A375细胞增殖方面比抑制剂更有效。
更新日期：2019-12-20
中文翻译：
MEK PROTAC的设计，合成和生物学评估。
已经基于变构MEK抑制剂设计了针对MEK降解的蛋白水解靶嵌合体（PROTAC）。用PROTAC抑制ERK1 / 2磷酸化的效果不如使用小分子抑制剂。然而，最好的PROTACs在抑制A375细胞增殖方面比抑制剂更有效。
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