Biomedical applications of radioiodinated peptides

The overexpression of peptide receptors in certain tumors as compared to endogeneous expression levels represents the molecular basis for the design of peptide-based tools for targeted nuclear imaging and therapy. Receptor targeting with radiolabelled peptides became a very important imaging and/or therapeutic approach in nuclear medicine and oncology. A great variety of peptides has been radiolabelled with clinical relevant radionuclides, such as radiometals and radiohalogens. However, to the best of our knowledge concise and updated reviews providing information about the biomedical application of radioiodinated peptides are still missing. This review outlines the synthetic efforts in the preparation of radioiodinated peptides highlighting the importance of radioiodine in nuclear medicine, giving an overview of the most relevant radioiodination strategies that have been employed and describes relevant examples of their use in the biomedical field. (C) 2019 Elsevier Masson SAS. All rights reserved.