Article
Inhibiting epidermal growth factor receptor at a distance.
Journal of the American Chemical Society - 13 Aug 2014
Sinclair Julie K-L, Denton Elizabeth V, Schepartz Alanna
Abstract excerpt
The epidermal growth factor receptor (EGFR) tyrosine kinase is implicated in a large number of human cancers. Most EGFR inhibitors target the extracellular, growth factor-binding domain or the intracellular, ATP-binding domain. Here we describe molecules that inhibit the kinase activity of EGFR in a new way, by competing with formation of an essential intradimer coiled coil containing the juxtamembrane segment...
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