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Published on: January 7, 2019
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[Development and Evaluation of At-211 Labeled Peptides]
1Graduate School of Medical Sciences, Kanazawa University.
Summary
Astatine-211 (211At) shows promise for targeted alpha therapy (TAT) due to its properties. This review covers developing 211At-labeled peptides, like RGD peptides, for potential radiotheranostics.
Area of Science:
- Nuclear medicine
- Radiochemistry
- Oncology
Background:
- Astatine-211 (211At) is a promising alpha-emitter for targeted alpha therapy (TAT).
- Its properties allow adaptation of radioiodination techniques for radiotheranostics.
- 211At's short half-life suits tumor-targeting molecules.
Purpose of the Study:
- To review the development of 211At-labeled peptides for TAT.
- To highlight the use of arginylglycylaspartic acid (RGD) peptide as a model targeting ligand.
Main Methods:
- Review of existing literature on 211At radiolabeling techniques.
- Focus on methods applicable to peptide labeling.
- Discussion of RGD peptide as a targeting moiety.
Main Results:
- 211At labeling is feasible using established radioiodination methods.
- Peptide-based targeting agents can be effectively labeled with 211At.
- RGD peptides demonstrate potential for 211At delivery to target sites.
Conclusions:
- 211At is a viable radionuclide for TAT, offering radiotheranostic potential.
- 211At-labeled peptides, such as RGD, are promising for targeted cancer therapy.
- Further development is needed to optimize 211At-based radiopharmaceuticals.

