title: An update of radiolabeled bombesin analogs for gastrin-releasing peptide receptor targeting.
abstract: Prostate cancer is a critical public health problem in USA and Europe. New non-invasive imaging methods are urgently needed, due to the low accuracy and specificity of current screen methods and the desire of localizing primary prostate cancer and bone metastasis. Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) are the non-invasive and sensitive imaging methods which have been widely used for diagnosing diseases in the clinic. Lack of suitable radiotracers is the major issue for nuclear imaging of prostate cancer, although radiolabeled bombesin (BN) peptides targeting the Gastrin-Releasing Peptide Receptor (GRPR) on tumor cells are widely investigated. In this review we discuss the recent trends in the development of GRPR-targeted radiopharmaceuticals based on BN analogs with regard to their potential for imaging and therapy of GRPR-expressing malignancies. Following a brief introduction of GRPR and bombesin peptides, we summarize the properties of prostate cancer specific radiolabeled bombesins. New bombesin tracers published in the last five years are reviewed and compared according to their novelties in biomolecules, radionuclides, labeling methods, bifunctional chelators and linkers. Hot topics such as multimerization, application of agonists and antagonists are highlighted in the review. Lastly, a few clinical trials of cancer nuclear imaging with radiolabeled bombesin have been discussed.
authors: Department of Nuclear Medicine and Molecular Imaging, University of Groningen, University Medical Center Groningen, Groningen, The Netherlands.
authors: Zilin
authors: Z
authors: Yu
authors: Hildo J K
authors: HJ
authors: Ananias
authors: Giuseppe
authors: G
authors: Carlucci
authors: Hilde D
authors: HD
authors: Hoving
authors: Wijnand
authors: W
authors: Helfrich
authors: Rudi A J O
authors: RA
authors: Dierckx
authors: Fan
authors: F
authors: Wang
authors: Igle J
authors: IJ
authors: de Jong
authors: Philip H
authors: PH
authors: Elsinga
mesh_terms: D000818:Animals; D001839:Bombesin / Q000031:analogs & derivatives; D001859:Bone Neoplasms / Q000000981:diagnostic imaging / Q000556:secondary; D015195:Drug Design; D006801:Humans; D008297:Male; D058990:Molecular Targeted Therapy; D049268:Positron-Emission Tomography / Q000379:methods; D011471:Prostatic Neoplasms / Q000000981:diagnostic imaging* / Q000188:drug therapy / Q000473:pathology; D019275:Radiopharmaceuticals; D018004:Receptors, Bombesin / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods
chemical_list: D019275:Radiopharmaceuticals; D018004:Receptors, Bombesin; D001839:Bombesin