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Author Spotlight: Evaluating Biophysical Assays for Characterizing PROTACS Ternary Complexes
Published on: January 12, 2024
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Design, Synthesis, and Biological Evaluation of MEK PROTACs
Stefan Vollmer, Danen Cunoosamy, Huafei Lv1
1Pharmaron Beijing Company, Limited , No. 6 Taihe Road, BDA , Beijing 100176 , P.R. China.
Journal of Medicinal Chemistry
|December 6, 2019
Abstract:
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.

