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Udgivet

Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

DOI

  1. Blocking of efflux transporters in rats improves translational validation of brain radioligands

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  2. Towards selective CNS PET imaging of the 5-HT7 receptor system: Past, present and future

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  3. Realizing Clinical Trials with Astatine-211: The Chemistry Infrastructure

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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.

OriginalsprogEngelsk
TidsskriftChemPlusChem
Vol/bind84
Udgave nummer7
Sider (fra-til)775-778
Antal sider4
ISSN2192-6506
DOI
StatusUdgivet - jul. 2019

Bibliografisk note

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

ID: 59320036