HER2介导抗癌药物传输：制备高特异性受体的靶向配体的策略

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:

关键词: 药物传递系统，HER2受体，筛选方法，选择性配体，合成受体片段，癌症靶向治疗

摘要: 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.

Cite this article as:

Enrica Calce, Luca Monfregola, Michele Saviano and Stefania De Luca , HER2-Mediated Anticancer Drug Delivery: Strategies to Prepare Targeting Ligands Highly Specific for the Receptor, Current Medicinal Chemistry 2015; 22 (21) . https://dx.doi.org/10.2174/0929867322666150521091103