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 for this work

1 Citation (Scopus)

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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.

Original language	English
Journal	ChemPlusChem
Volume	219
Issue number	84
Pages (from-to)	775-778
Number of pages	4
ISSN	2192-6506
DOIs	https://doi.org/10.1002/cplu.201900114
Publication status	Published - 1 Jan 2019

Keywords

bioorthogonal chemistry
click chemistry
multicomponent reactions
radiochemistry
radiolabeling

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10.1002/cplu.201900114Licence: CC BY-NC

Denk_et_al-2019-ChemPlusChemFinal published version, 1.44 MBLicence: CC BY-NC

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title = "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 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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T1 - Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking

AU - Denk, Christoph

AU - Wilkovitsch, Martin

AU - Aneheim, Emma

AU - Herth, Matthias M.

AU - Jensen, Holger

AU - Lindegren, Sture

AU - Mikula, Hannes

PY - 2019/1/1

Y1 - 2019/1/1

N2 - 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.

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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DO - 10.1002/cplu.201900114

M3 - Journal article

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AN - SCOPUS:85063866669

SN - 2192-6506

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EP - 778

JO - ChemPlusChem

JF - ChemPlusChem

IS - 84

ER -

Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking

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