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Updated: May 25, 2026
Preparation and Evaluation of 99mTc-labeled Tridentate Chelates for Pre-targeting Using Bioorthogonal Chemistry
Published on: February 4, 2017
Chelating systems for (99m)Tc/(188)Re in the development of radiolabeled peptide pharmaceuticals
Cristina Bolzati1, Davide Carta, Nicola Salvarese
1ICIS-CNR, Corso Stati Uniti, 4, 35127 Padova, Italy. refosco@icis.cnr.it
Abstract:
Currently, receptor based radiopharmaceuticals have received great attention in molecular imaging and radiotherapy of cancer, and provide a unique tool for target-specific delivery of radionuclides to pathological tissues. In this context, receptor binding peptides represent an attractive class of target vectors for Nuclear Medicine purposes. The rich chemistry of the group 7 elements elaborated in past years, has allowed the development of different procedures for the preparation of radiolabeled peptides in high yield. This, joint to the use of solid-phase peptide synthesis, has opened the possibility to explore new strategies for approaching the design of new class of radiolabeled receptor-targeted peptides, and to create new versatilities in targeting vehicle design e.g. in synthesis of metal-cyclized peptides or of multivalent targeting agents. This review provides an overview on several aspects of the development of new (99m)Tc/(188)Re-peptide based target specific radiopharmaceuticals, in particular on the synthetic strategies employed for modifying molecular vectors, and the application of the different metal-cores and/or building block for preparing high specific activity agents.
Insights
Receptor-targeted radiopharmaceuticals using technetium-99m (99mTc) and rhenium-188 (188Re) peptides offer precise cancer imaging and therapy. Advances in peptide synthesis and radiolabeling enable new targeted drug delivery strategies.
Area of Science:
- Nuclear Medicine
- Radiopharmaceutical Chemistry
- Molecular Imaging
Background:
- Receptor-based radiopharmaceuticals are crucial for targeted cancer imaging and radiotherapy.
- Peptide vectors are attractive for delivering radionuclides to specific pathological tissues.
- Group 7 element chemistry facilitates high-yield radiolabeled peptide preparation.
Purpose of the Study:
- To review the development of novel (99m)Tc/(188)Re-peptide based radiopharmaceuticals.
- To highlight synthetic strategies for modifying molecular targeting vectors.
- To discuss the application of various metal-cores and building blocks for high specific activity agents.
Main Methods:
- Solid-phase peptide synthesis.
- Development of radiolabeling procedures for group 7 elements.
- Design of metal-cyclized peptides and multivalent targeting agents.
Main Results:
- Established synthetic strategies for modifying molecular vectors.
- Explored versatile targeting vehicle designs, including metal-cyclized and multivalent agents.
- Demonstrated the utility of different metal-cores and building blocks for high specific activity agents.
Conclusions:
- Peptide-based radiopharmaceuticals offer a versatile platform for targeted cancer therapy and diagnosis.
- Advancements in synthetic chemistry enable the creation of sophisticated radiolabeled targeting agents.
- Further development in this field promises improved precision in molecular imaging and radiotherapy.
