Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking

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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 languageEnglish
JournalChemPlusChem
Volume219
Issue number84
Pages (from-to)775-778
Number of pages4
ISSN2192-6506
DOIs
Publication statusPublished - 1 Jan 2019

    Research areas

  • bioorthogonal chemistry, click chemistry, multicomponent reactions, radiochemistry, radiolabeling

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