2. Academic Validation
  3. Design, Synthesis, and Biological Evaluation of MEK PROTACs

Design, Synthesis, and Biological Evaluation of MEK PROTACs

  • J Med Chem. 2020 Jan 9;63(1):157-162. 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
Affiliations

Affiliation

  • 1 Pharmaron Beijing Company, Limited , No. 6 Taihe Road, BDA , Beijing 100176 , P.R. China.
PMID: 31804822 DOI: 10.1021/acs.jmedchem.9b00810
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.

Figures
Products