Sara J Khosrowjerdi
21 - Designing Cyclic Peptide Inhibitors of Eps15
Epidermal growth factor pathway substrate 15 (Eps15) is substrate for the kinase activity of the epidermal growth factor receptor (EGFR), a validated cancer target. Eps15 is required for EGFR internalization. The Eps15 homology (EH) domain is a protein interaction module first identified in Eps15. Genetic studies have implicated EH domains in the internalization and recycling of EGFR to the cell membrane. Though EH domains have been identified in over 20 proteins involved in vesicle trafficking and endocytosis pathways, there are no useful molecular inhibitors for these domains. Such inhibitors will be important tools for biological investigation of vesicle trafficking and for validating EH-domain-containing proteins as potential pharmacological targets. This project aims to design cyclic peptides inhibitors of the EH domains of Eps15 as a necessary tool for scientific discovery..