From Bench to Bed: New Gastrin-Releasing Peptide Receptor-Directed Radioligands and Their Use in Prostate Cancer.

Gastrin-releasing peptide receptors (GRPRs) are overexpressed in prostate and breast cancer, and are therefore attractive molecular targets for diagnosis and therapy with radiolabeled GRPR-directed peptide probes. The amphibian tetradecapeptide bombesin or the mammalian gastrin-releasing peptide and neuromedin C have been modified with a variety of chelators. As a result, labeling with radiometals attractive for SPECT or PET imaging and for radionuclide therapy has led to the development of peptide radioligands suitable for in vivo targeting of prostate cancer. A shift of paradigm from internalizing GRPR-agonists to antagonists has occurred owing to the higher biosafety and superior pharmacokinetics of radioantagonists.