Peptide-Based Positron Emission Tomography Probes: Current Strategies for Synthesis and radiolabelling

Mariacristina Failla; Giuseppe Floresta; Vincenzo Abbate

doi:10.1039/D2MD00397J

Peptide-Based Positron Emission Tomography Probes: Current Strategies for Synthesis and radiolabelling

Mariacristina Failla, Giuseppe Floresta, Vincenzo Abbate

Research output: Contribution to journal › Review article › peer-review

13 Citations (Scopus)

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Abstract

In medical imaging, techniques such as magnetic resonance imaging, contrast-enhanced computerized tomography, and positron emission tomography (PET) are extensively available and routinely used for disease diagnosis and treatment. Peptide-based targeting PET probes are usually small peptides with high affinity and specificity to specific cellular and tissue targets opportunely engineered for acting as PET probes. For instance, either the radioisotope (e.g., ¹⁸F, ¹¹C) can be covalently linked to the peptide-probe or another ligand that strongly complexes the radioisotope (e.g., ⁶⁴Cu, ⁶⁸Ga) through multiple coordinative bonds can be chemically conjugated to the peptide delivery moiety. The main advantages of these probes are that they are cheaper than classical antibody-based PET tracers and can be efficiently chemically modified to be radiolabelled with virtually any radionuclide making them very attractive for clinical use. The goal of this review is to report and summarize recent technologies in peptide PET-based molecular probes synthesis and radiolabelling with the most used radioisotopes in 2022.

Original language	English
Pages (from-to)	592-623
Number of pages	32
Journal	RSC Medicinal Chemistry
Volume	14
Issue number	4
Early online date	6 Jan 2023
DOIs	https://doi.org/10.1039/D2MD00397J
Publication status	Published - 6 Jan 2023

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Peptide-based positron_FAILLA_Publishedonline6January2023_GOLD VoR (CC BY)Final published version, 876 KBLicence: CC BY

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title = "Peptide-Based Positron Emission Tomography Probes: Current Strategies for Synthesis and radiolabelling",

abstract = "In medical imaging, techniques such as magnetic resonance imaging, contrast-enhanced computerized tomography, and positron emission tomography (PET) are extensively available and routinely used for disease diagnosis and treatment. Peptide-based targeting PET probes are usually small peptides with high affinity and specificity to specific cellular and tissue targets opportunely engineered for acting as PET probes. For instance, either the radioisotope (e.g., 18F, 11C) can be covalently linked to the peptide-probe or another ligand that strongly complexes the radioisotope (e.g., 64Cu, 68Ga) through multiple coordinative bonds can be chemically conjugated to the peptide delivery moiety. The main advantages of these probes are that they are cheaper than classical antibody-based PET tracers and can be efficiently chemically modified to be radiolabelled with virtually any radionuclide making them very attractive for clinical use. The goal of this review is to report and summarize recent technologies in peptide PET-based molecular probes synthesis and radiolabelling with the most used radioisotopes in 2022.",

author = "Mariacristina Failla and Giuseppe Floresta and Vincenzo Abbate",

note = "Funding Information: This project has received funding from the European Union's Horizon 2020 Research and Innovation Program under Grant agreement no 893784. Publisher Copyright: {\textcopyright} 2023 RSC.",

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AU - Failla, Mariacristina

AU - Floresta, Giuseppe

AU - Abbate, Vincenzo

PY - 2023/1/6

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N2 - In medical imaging, techniques such as magnetic resonance imaging, contrast-enhanced computerized tomography, and positron emission tomography (PET) are extensively available and routinely used for disease diagnosis and treatment. Peptide-based targeting PET probes are usually small peptides with high affinity and specificity to specific cellular and tissue targets opportunely engineered for acting as PET probes. For instance, either the radioisotope (e.g., 18F, 11C) can be covalently linked to the peptide-probe or another ligand that strongly complexes the radioisotope (e.g., 64Cu, 68Ga) through multiple coordinative bonds can be chemically conjugated to the peptide delivery moiety. The main advantages of these probes are that they are cheaper than classical antibody-based PET tracers and can be efficiently chemically modified to be radiolabelled with virtually any radionuclide making them very attractive for clinical use. The goal of this review is to report and summarize recent technologies in peptide PET-based molecular probes synthesis and radiolabelling with the most used radioisotopes in 2022.

AB - In medical imaging, techniques such as magnetic resonance imaging, contrast-enhanced computerized tomography, and positron emission tomography (PET) are extensively available and routinely used for disease diagnosis and treatment. Peptide-based targeting PET probes are usually small peptides with high affinity and specificity to specific cellular and tissue targets opportunely engineered for acting as PET probes. For instance, either the radioisotope (e.g., 18F, 11C) can be covalently linked to the peptide-probe or another ligand that strongly complexes the radioisotope (e.g., 64Cu, 68Ga) through multiple coordinative bonds can be chemically conjugated to the peptide delivery moiety. The main advantages of these probes are that they are cheaper than classical antibody-based PET tracers and can be efficiently chemically modified to be radiolabelled with virtually any radionuclide making them very attractive for clinical use. The goal of this review is to report and summarize recent technologies in peptide PET-based molecular probes synthesis and radiolabelling with the most used radioisotopes in 2022.

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Peptide-Based Positron Emission Tomography Probes: Current Strategies for Synthesis and radiolabelling

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