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Radiolabeled GRPR Antagonists for Imaging of Disseminated Prostate Cancer. Influence of Labeling Chemistry on Targeting Properties


Bogdan Mitran, Vladimir Tolmachev * and Anna Orlova   Pages 1 - 22 ( 22 )


Background: Radionuclide molecular imaging of gastrin-releasing peptide receptor (GRPR) expression promises unparalleled opportunities for visualizing subtle prostate tumors, which due to small size, adjacent benign tissue, or a challenging location would otherwise remain undetected by conventional imaging. Achieving high imaging contrast is essential for this purpose and the molecular design of any probe for molecular imaging of prostate cancer should be aimed at obtaining as high tumor-to-organ ratios as possible.

Objective: This short review summarizes the key imaging modalities currently used in prostate cancer, with a special focus on radionuclide molecular imaging. Emphasis is laid mainly on the issue of radiometals labeling chemistry and its influence on the targeting properties and biodistribution of radiolabeled GRPR antagonists for imaging of disseminated prostate cancer.

Methods: A comprehensive literature search of the PubMed/MEDLINE, and Scopus library databases was conducted to find relevant articles.

Results: The combination of radionuclide, chelator and required labeling chemistry was shown to have a significant influence on the stability, binding affinity, and internalization rate, off-target interaction with normal tissues and blood proteins, interaction with enzymes, activity uptake and retention in excretory organs and activity uptake in tumors of radiolabeled bombesin antagonistic analogues.

Conclusion: Labeling chemistry had a very strong impact on the biodistribution profile of GRPR-targeting peptide based imaging probes and needs to be considered when designing a targeting probe for high contrast molecular imaging. Taking into account the complexity of in vivo interactions, it is not currently possible to accurately predict the optimal labeling approach. Therefore, a detailed characterization and optimization is essential for the rational design of imaging agents.


Prostate cancer, molecular imaging, gastrin-releasing peptide receptor, GRPR antagonist, radiolabeling.


Uppsala University, Department of Medicianl Chemistry, Faculty of Pharmacy, Uppsala University,Faculty of Medicine, Department of Immunology, Genetics and Pathology, Uppsala University, Department of Medicianl Chemistry, Faculty of Pharmacy

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