Transmembrane Domain Targeting Peptide Antagonizing ErbB2/Neu Inhibits Breast Tumor Growth and Metastasis

摘要: Breast cancer is still a deadly disease despite major achievements in targeted therapies designed to block ligands or ligand-binding subunits of tyrosine kinase receptors. Relapse significant and metastases deleterious, which demands novel strategies for fighting this disease. Here, we report proof-of-concept experiment demonstrating that small peptides interfering with the transmembrane domain epidermal growth factor receptor ErbB2 exhibit anticancer properties when used at micromolar dosages genetically engineered mouse model breast cancer. Different assays demonstrate specificity ErbB2-targeting peptide, induces long-term reduction phosphorylation Akt signaling consistent reduced tumor cell proliferation increased survival. Microcomputed tomography analysis established antimetastatic activity peptide its impact on primary growth. This reveals interior membrane as an unexplored dimension drug design.