Beta-Peptide Inhibitors of Protein-Protein Interactions

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DESCRIPTION (provided by applicant): Protein-protein interactions are of great importance in cell function and, consequently, as targets for medicinal chemistry. Where traditional small-molecule based drug design has proven ineffective in the development of antagonists of certain interactions, macromolecular approaches are finding increasing utility. Human epidermal growth factor receptor (EGFR) is a membrane bound cell surface receptor the malfunction of which is linked to a number of cancers. We propose to identify beta-peptide foldamers capable of modulating EGFR function by mimicking protein surfaces involved in receptor dimerization. This project will allow us to explore the scope and limitations of beta-peptide scaffolds as mimics of natural protein surfaces and could lead to the development of new anticancer therapeutics.