Abstract
The high incidence of prostate cancer (PCa) increases the need for progress in its diagnosis, staging, and precise treatment. The overexpression of tumor-specific receptors for peptides in human cancer cells, such as gastrin-releasing peptide receptor, natriuretic peptide receptor, and somatostatin receptor, has indicated the ideal molecular basis for targeted imaging and therapy. Targeting these receptors using radiolabeled peptides and analogs have been an essential topic on the current forefront of PCa studies. Radiolabeled peptides have been used to target receptors for molecular imaging in human PCa with high affinity and specificity. The radiolabeled peptides enable optimal quick elimination from blood and normal tissues, producing high contrast for positron emission computed tomography and single-photon emission computed tomography imaging with high tumor-to-normal tissue uptake ratios. Owing to their successful application in visualization, peptide derivatives with therapeutic radionuclides for peptide receptor radionuclide therapy in PCa have been explored in recent years. These developments offer the promise of personalized, molecular medicine for individual patients. Hence, we review the preclinical and clinical literature in the past 20 years and focus on the newer developments of peptide-based radiopharmaceuticals for the imaging and therapy of PCa.
Highlights
Prostate cancer (PCa) is the most common sex-related malignancy and second most common cause of mortality after lung cancer, accounting for 10% of all tumors in men (Siegel et al, 2020)
It is known that prostate tumors arise primarily in the peripheral zone (PZ) of the prostate and 20–30% often originated in the transition zone (TZ)
Great efforts have been made in the development of peptidebased radiopharmaceuticals for PCa diagnosis and radiotherapy
Summary
Prostate cancer (PCa) is the most common sex-related malignancy and second most common cause of mortality after lung cancer, accounting for 10% of all tumors in men (Siegel et al, 2020). Prostate-specific antigen (PSA) is generally used as an important clinical marker of early diagnosis, clinical stage, and postoperative observation for PCa because the PSA levels can rise before the presence of detectable PCa recurrence (Dall’oglio et al, 2005; Van Poppel et al, 2006) This marker does not help localize and differentiate the disease. Overexpressed prostate tumor-specific receptors are detected on the cell surface and play an important role in different stages of carcinogenesis and metastasis. Design and development of peptide-based radiopharmaceuticals for targeted molecular imaging or therapy in oncology include radionuclides with appropriate emission characteristics, metal complexing agents, pharmacokinetic modifiers, and receptorspecific targeting peptides (Figure 1). Fluorine-18 Gallium-68 Indium-111 Technetium-99m Yttrium-86 Copper-64 Lutetium-177 Yttrium-90
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