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Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking.

ABSTRACT: 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.

SUBMITTER: Denk C

PROVIDER: S-EPMC6813637 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature

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Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking.

Denk Christoph C Wilkovitsch Martin M Aneheim Emma E Herth Matthias M MM Jensen Holger H Lindegren Sture S Mikula Hannes H

ChemPlusChem 20190404 7

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. T ...[more]

PMID: 31681526

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