title: Radiolabeled bombesin derivatives for preclinical oncological imaging.
abstract: Despite efforts, cancer is still one of the leading causes of morbidity and mortality worldwide, with approximately 14 million new cases and 8.2 million cancer-related deaths each year, according to the World Health Organization. Among the strategies to reduce cancer progression and improving its management, implementing early detection technologies is crucial. Based on the fact that several types of cancer cells overexpress surface receptors, small molecule ligands, such as peptides, have been developed to allow tumor identification at earlier stages. Allied with imaging techniques such as PET and SPECT, radiolabeled peptides play a pivotal role in nuclear medicine. Bombesin, a peptide of 14 amino acids, is an amphibian homolog to the mammalian gastrin-releasing peptide (GRP), that has been extensively studied as a targeting ligand for diagnosis and therapy of GRP positive tumors, such as breast, pancreas, lungs and prostate cancers. In this context, herein we provide a review of reported bombesin derivatives radiolabeled with a multitude of radioactive isotopes for diagnostic purposes in the preclinical setting. Moreover, since animal models are highly relevant for assessing the potential of clinical translation of this radiopeptides, a brief report of the currently used GRP-positive tumor-bearing animal models is described.
authors.affiliation: Biomedical Engineering Program, University of Wisconsin-Madison, Madison, WI 53705, USA.
authors.forename: Carolina de Aguiar
authors.initials: CA
authors.lastname: Ferreira
authors.affiliation: Faculty of Pharmacy, Federal University of Minas Gerais, Av. Antônio Carlos, 6627, 31270-901, Belo Horizonte, Minas Gerais, Brazil.
authors.forename: Leonardo Lima
authors.initials: LL
authors.lastname: Fuscaldi
authors.affiliation: Department of Drug Discovery and Pharmaceutical Sciences, Medical University of South Carolina, USA.
authors.forename: Danyelle M
authors.initials: DM
authors.lastname: Townsend
authors.affiliation: Department of Nuclear Medicine, Radiology, NeuroRadiology, Medical Physics, Clinical Laboratory, Microbiology, Pathology, Santa Maria della Misericordia Hospital, Rovigo, Italy. Electronic address: domenico.rubello@libero.it.
authors.forename: Domenico
authors.initials: D
authors.lastname: Rubello
authors.affiliation: Faculty of Pharmacy, Federal University of Minas Gerais, Av. Antônio Carlos, 6627, 31270-901, Belo Horizonte, Minas Gerais, Brazil.
authors.forename: André Luís Branco de
authors.initials: ALB
authors.lastname: Barros
mesh_terms: D000818:Animals; D001839:Bombesin / Q000378:metabolism*; D003952:Diagnostic Imaging / Q000379:methods / Q000639:trends*; D006801:Humans; D009369:Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism*; D049268:Positron-Emission Tomography / Q000379:methods / Q000639:trends; D019275:Radiopharmaceuticals / Q000378:metabolism*; D018004:Receptors, Bombesin / Q000096:biosynthesis; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods / Q000639:trends
chemical_list: D019275:Radiopharmaceuticals; D018004:Receptors, Bombesin; D001839:Bombesin
keywords: Molecular imaging; Oncological imaging; PET imaging; Preclinical data; Radiolabeled bombesin derivatives; SPECT imaging