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 GRPRtargeted
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
Keywords: Bombesin, GRPR, prostate cancer, bone metastasis, PET, SPECT, targeting, imaging.
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