Receptor-mediated tumor targeting with radiopeptides

Abstract

Radiolabeled peptides have become important tools for preclinical cancer research, and in nuclear oncology they serve as diagnostic and more recently also as therapeutic agents. In the latter application, radiolabeled peptides represent a distinct sector of the molecular targeting approach, which in many areas of therapy implements the old “magic bullet” concept by specifically directing the therapeutic agent to the site of action. Although in the past few years the development of receptor-mediated targeting for therapy has been confined to some radiolabeled antibodies and to somatostatin/SRIF, research into an increasing number of radiolabeled peptides and their receptors expressed by different tumors will soon lead to a wider use of peptide radiopharmaceuticals. In a consecutive series of six reviews we present a comprehensive overview of the literature on receptor-mediated tumor targeting with the different radiopeptides currently studied. Part 1 summarizes the concepts and methods of radiopeptide targeting, the selection of radioisotopes, chelators, the critera of peptide ligand development and some general aspects of diagnostic and therapeutic application of peptide radiopharmaceuticals.

Keywords::

• Molecular targeting
• tumor
• receptor
• peptide
• radioisotope
• chelator
• scintigraphy
• radiopharmaceutical

Acknowledgments

We thank the Swiss Cancer League and the Swiss National Science Foundation for financial support.

Declaration of interest: The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.