期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 63, 期 1, 页码 157-162出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.9b00810
关键词
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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.
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