title: From Bench to Bed: New Gastrin-Releasing Peptide Receptor-Directed Radioligands and Their Use in Prostate Cancer.
abstract: 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.
authors.affiliation: Molecular Radiopharmacy, INRASTES, NCSR "Demokritos", Agia Paraskevi, Attikis, Athens 15310, Greece. Electronic address: maina_thea@hotmail.com.
authors.forename: Theodosia
authors.initials: T
authors.lastname: Maina
authors.affiliation: Molecular Radiopharmacy, INRASTES, NCSR "Demokritos", Agia Paraskevi, Attikis, Athens 15310, Greece.
authors.forename: Berthold A
authors.initials: BA
authors.lastname: Nock
mesh_terms: D000595:Amino Acid Sequence; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005544:Forecasting; D006801:Humans; D008297:Male; D000072078:Positron Emission Tomography Computed Tomography / Q000379:methods / Q000639:trends; D011471:Prostatic Neoplasms / Q000000981:diagnostic imaging*; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D018004:Receptors, Bombesin / Q000037:antagonists & inhibitors / Q000378:metabolism*
chemical_list: D011868:Radioisotopes; D019275:Radiopharmaceuticals; D018004:Receptors, Bombesin
keywords: Clinical translation; Gastrin-releasing peptide receptor targeting; Preclinical design; Prostate cancer; Theranostics