Title:HER2-Mediated Anticancer Drug Delivery: Strategies to Prepare Targeting Ligands Highly Specific for the Receptor
Volume: 22
Issue: 21
Author(s): Enrica Calce, Luca Monfregola, Michele Saviano and Stefania De Luca
Affiliation:
Keywords:
Drug delivery systems, HER2 receptor, Screening methods, Selective ligand, Synthetic receptor fragment, Targeted
cancer therapy.
Abstract: HER2 receptor, for its involvement in tumorigenesis, has been largely studied
as topic in cancer research. In particular, the employment of trastuzumab (Herceptin),
a humanized anti-HER2 antibody, showed several clinical benefits in the therapy
against the breast cancer. Moreover, for its accessible extracellular domain, this
receptor is considered an ideal target to deliver anticancer drugs for the receptormediated
anticancer therapy. By now, monoclonal antibody and its fragments, affibody, and some peptides have been employed
as targeting agents in order to deliver various drugs to HER2 positive tumor cells. In particular, the ability to perform
a fast and reliable screening of a large number of peptide molecules would make possible the selection of highly
specific compounds to the receptor target. In this regard, the availability of preparing a simplified synthetic model which
is a good mimetic of the receptor target and can be used in a reliable screening method of ligands would be of a strategic
importance for the development of selective HER2-targeting peptide molecules. Herein, we illustrate the importance of
HER2-targeted anticancer therapies. We also report on a synthetic and effective mimetic of the receptor, which revealed
to be a useful tool for the selection of specific HER2 ligands.
