Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking

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Christoph Denk, Martin Wilkovitsch, Emma Aneheim, Matthias M. Herth, Holger Jensen, Sture Lindegren, Hannes Mikula

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
Issue number84
Pages (from-to)775-778
Number of pages4
Publication statusPublished - 1 Jan 2019

    Research areas

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

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