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卷 16, 期 18, 页码 4916-4919出版社
AMER CHEMICAL SOC
DOI: 10.1021/ol502426b
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- NIH [GM 83257]
The hydrocarbon-stapled peptide E1(S) allosterically inhibits the kinase activity of the epidermal growth factor receptor (EGFR) by blocking a distant but essential protein protein interaction: a coiled coil formed from the juxtamembrane segment (JM) of each member of the dimeric partnership.(1) Macrocyclization is not required for activity: the analogous unstapled (but alkene-bearing) peptide is equipotent in cell viability, immunoblot, and bipartite display experiments to detect coiled coil formation on the cell surface.
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