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Published on: January 7, 2019
Peptides in receptor-mediated radiotherapy: from design to the clinical application in cancers
Catherine Lozza1, Isabelle Navarro-Teulon, André Pèlegrin
1Institut de Recherche en Cancérologie de Montpellier , Montpellier , France ; INSERM, U896 , Montpellier , France ; Université Montpellier 1 , Montpellier , France ; Institut Régional du Cancer Montpellier , Montpellier , France.
Abstract:
Short peptides can show high affinity for specific receptors overexpressed on tumor cells. Some of these are already used in cancerology as diagnostic tools and others are in clinical trials for therapeutic applications. Therefore, peptides exhibit great potential as a diagnostic tool but also as an alternative or an additional antitumoral approach upon the covalent attachment of a therapeutic moiety such as a radionuclide or a cytotoxic drug. The chemistry offers flexibility to graft onto the targeting-peptide either fluorine or iodine directly, or metallic radionuclides through appropriate chelating agent. Since short peptides are straightforward to synthesize, there is an opportunity to further improve existing peptides or to design new ones for clinical applications. However, several considerations have to be taken into account to optimize the recognition properties of the targeting-peptide to its receptor, to improve its stability in the biological fluids and its residence in the body, or to increase its overall therapeutic effect. In this review, we highlight the different aspects which need to be considered for the development of an efficient peptide receptor-mediated radionuclide therapy in different neoplasms.
Insights
Short peptides targeting tumor receptors show promise for cancer diagnosis and therapy. Optimizing peptide design is key for effective peptide receptor-mediated radionuclide therapy in neoplasms.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging
Background:
- Short peptides exhibit high affinity for tumor-specific receptors.
- Peptides are utilized as diagnostic tools and therapeutic agents in cancer treatment.
- Peptide-based strategies offer potential for targeted cancer therapy.
Purpose of the Study:
- To review the development of peptide receptor-mediated radionuclide therapy (PRMNT).
- To highlight key considerations for optimizing PRMNT efficacy.
- To discuss the potential of peptides in cancer diagnostics and therapeutics.
Main Methods:
- Review of current literature on peptide targeting in oncology.
- Analysis of chemical strategies for peptide modification and radionuclide conjugation.
- Discussion of factors influencing peptide stability, biodistribution, and therapeutic effect.
Main Results:
- Peptides can be functionalized with diagnostic or therapeutic moieties (e.g., radionuclides, cytotoxic drugs).
- Chemical synthesis allows for peptide optimization and novel design.
- Several factors require careful consideration for successful PRMNT development.
Conclusions:
- Peptides are versatile tools for cancer diagnosis and therapy.
- Further optimization of peptide properties is crucial for enhancing PRMNT.
- Peptide receptor-mediated radionuclide therapy holds significant potential for treating various neoplasms.
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