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- W2006013753 abstract "The epidermal growth factor receptor (EGFR) is overexpressed in multiple carcinomas and is the focus of a variety of targeted therapies. Here we report the design of peptide-based compounds that mimic the EGFR dimerization arm and inhibit allosteric activation of EGFR. These peptides are modified to contain a triazolyl bridge between the peptide strands to constrain the EGFR dimerization arm β-loop. In this study, we demonstrate that these peptides have significantly improved proteolytic stability over the non-modified peptide sequence, and their inhibitory effects are dependent on the number of the methylene units and orientation of the introduced triazolyl bridge. We identified a peptide, EDA2, which downregulates receptor phosphorylation and dimerization and reduces cell viability. This is the first example of a biologically active triazolyl-bridged peptide targeting the EGFR dimerization interface that effectively downregulates EGFR activation." @default.
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- W2006013753 date "2015-03-19" @default.
- W2006013753 modified "2023-10-16" @default.
- W2006013753 title "Inhibiting EGFR Dimerization Using Triazolyl-Bridged Dimerization Arm Mimics" @default.
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- W2006013753 doi "https://doi.org/10.1371/journal.pone.0118796" @default.
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