Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking
Research output: Contribution to journal › Journal article › Research › peer-review
Documents
- Denk_et_al-2019-ChemPlusChem
Final published version, 1.44 MB, PDF document
In the past decade, several developments have expanded the chemical toolbox for astatination and the preparation of 211 At-labeled radiopharmaceuticals. However, there is still a need for advanced methods for the synthesis of astatinated (bio)molecules to address challenges such as limited in vivo stability. Herein, we report the development of multifunctional 211 At-labeled reagents that can be prepared by applying a modular and versatile click approach for rapid assembly. The introduction of tetrazines as bioorthogonal tags enables rapid radiolabeling and radio-crosslinking, which is demonstrated by steric shielding of 211 At to significantly increase label stability in human blood plasma.
Original language | English |
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Journal | ChemPlusChem |
Volume | 219 |
Issue number | 84 |
Pages (from-to) | 775-778 |
Number of pages | 4 |
ISSN | 2192-6506 |
DOIs | |
Publication status | Published - 1 Jan 2019 |
- bioorthogonal chemistry, click chemistry, multicomponent reactions, radiochemistry, radiolabeling
Research areas
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