Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking

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

doi:10.1002/cplu.201900114

Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking

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

^*Corresponding author af dette arbejde

1 Citationer (Scopus)

23 Downloads (Pure)

Abstract

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.

Originalsprog	Engelsk
Tidsskrift	ChemPlusChem
Vol/bind	219
Udgave nummer	84
Sider (fra-til)	775-778
Antal sider	4
ISSN	2192-6506
DOI	https://doi.org/10.1002/cplu.201900114
Status	Udgivet - 1 jan. 2019

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10.1002/cplu.201900114Licens: CC BY-NC

Denk_et_al-2019-ChemPlusChemForlagets udgivne version, 1,44 MBLicens: CC BY-NC

Citationsformater

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abstract = " 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. ",

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AU - Denk, Christoph

AU - Wilkovitsch, Martin

AU - Aneheim, Emma

AU - Herth, Matthias M.

AU - Jensen, Holger

AU - Lindegren, Sture

AU - Mikula, Hannes

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AB - 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.

KW - bioorthogonal chemistry

KW - click chemistry

KW - multicomponent reactions

KW - radiochemistry

KW - radiolabeling

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SP - 775

EP - 778

JO - ChemPlusChem

JF - ChemPlusChem

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Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking

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