Ontology highlight
ABSTRACT:
SUBMITTER: Sinclair JK
PROVIDER: S-EPMC4140499 | biostudies-literature | 2014 Aug
REPOSITORIES: biostudies-literature
Sinclair Julie K-L JK Denton Elizabeth V EV Schepartz Alanna A
Journal of the American Chemical Society 20140730 32
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 from each member of the receptor partnership. The most potent molecules we describe bi ...[more]