Let it bind: cyclization of Mig-6 segment 2 to target EGFR signaling in lung cancer

AbstractActivation of epidermal growth factor receptor signaling by kinase dimerization plays a crucial role in the development, progression, and metastasis of lung cancer. Tumor suppressor Mig-6 is a natural inhibitory protein of epidermal growth factor receptor signaling; the protein uses its two regions, namely segments 1 and 2, to directly interact with kinase dimerization interface and then inactivates the kinases. Here, we attempted to improve the binding capability of isolated segment 2 peptide to epidermal growth factor receptor family kinases by cyclizing the peptide. In the procedure, a disulfide bond was introduced across two ends of the peptide to constrain the peptide conformation in an antiparallel, double-strandedβ-sheet. Molecular dynamics simulations indicated high-struct...

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