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Development of a 68Gallium-Labeled D-Peptide PET Tracer for Imaging Programmed Death-Ligand 1 Expression
Published on: February 3, 2023
Application of radiolabeled peptides in tumor imaging and therapy
Naser Mohtavinejad1, Mehdi Shafiee Ardestani1, Ali Khalaj2
1Department of Radiopharmacy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
Abstract:
Scientists are looking for new therapies to cope with the rise in cancer worldwide. Since cancer cells overexpress peptide receptors and owing to small size, easy uptake by tumor cells, easy preparation, and with no toxicity, the use of radiolabeled peptides with high specificity and affinity for accurate imaging and therapy has attracted much attention. To develop an ideal imaging or treatment radiolabeled peptide, there are some aspects in the components of radiolabeled peptide including radionuclide, peptide, chelator, and spacer that should be considered. Some peptides, including somatostatin, RGD, neurotensin, bombesin, exendin, vasoactive intestinal peptide, and gastrin are currently under (pre)clinical investigations. Today, nanoparticles are suitable tools for targeting peptide for molecular imaging and therapy of tumors with low toxicity. This paper presents some essential aspects in developing a valuable radiolabeled peptide and some radiolabeled peptides with regard to their applications in tumor imaging and therapy in pre-clinical and clinical phases.
Insights
Radiolabeled peptides offer promising cancer therapies due to tumor cell uptake and low toxicity. This review covers key components and applications of these targeted radiopharmaceuticals for imaging and treatment.
Area of Science:
- Oncology
- Radiopharmaceutical Chemistry
- Molecular Imaging
- Cancer Therapy
Background:
- Rising global cancer incidence necessitates novel therapeutic strategies.
- Cancer cells' overexpression of peptide receptors makes them ideal targets.
- Radiolabeled peptides offer high specificity and affinity for tumor targeting.
Purpose of the Study:
- To review essential aspects of developing effective radiolabeled peptides for cancer.
- To discuss current (pre)clinical applications of various radiolabeled peptides.
- To highlight the role of nanoparticles in targeted peptide delivery for oncology.
Main Methods:
- Review of essential components: radionuclide, peptide, chelator, and spacer.
- Analysis of peptide selection based on receptor expression and targeting.
- Consideration of nanoparticle-based delivery systems for enhanced efficacy.
Main Results:
- Several peptides (somatostatin, RGD, neurotensin, bombesin, exendin, VIP, gastrin) are under investigation.
- Radiolabeled peptides demonstrate potential in both tumor imaging and therapy.
- Nanoparticles enhance targeting and reduce toxicity of peptide-based agents.
Conclusions:
- Radiolabeled peptides are valuable tools for precise tumor imaging and targeted therapy.
- Careful consideration of peptide, radionuclide, chelator, and spacer is crucial for optimal design.
- Continued research and development, including nanoparticle integration, promise improved cancer treatment outcomes.
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