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Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review


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Vis graf over relationer

In the past decade, several developments have expanded the chemical toolbox for astatination and the preparation of 211At-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 211At-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 211At to significantly increase label stability in human blood plasma.

Udgave nummer7
Sider (fra-til)775-778
Antal sider4
StatusUdgivet - jul. 2019

Bibliografisk note

© 2019 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA.

ID: 59320036