Development of Targeting Ligands for HER2 Receptor: Simplified Receptor Model Employed for Selecting Highly Specific Molecules

The interaction between Herceptin (Fab)-derived dimeric peptide and HER2-DIVMP, a synthetic peptide mimicking the subdomain IV of the receptor HER2, was monitored by fluorescence spectroscopy method. The obtained results confirmed that the adopted mimetic receptor fragment represents a reliable model system to monitor the ability of selected ligands to bind the receptor target, avoiding the involvement of cells or cellular extracts in a preliminary binding assay. Moreover, HER2-DIVMP has the characteristics of being easily integrated in rapid, efficient and inexpensive screening method for optimizing small molecules as targeting ligands for the receptor-mediated anticancer therapy.