Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking
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Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking. / Denk, Christoph; Wilkovitsch, Martin; Aneheim, Emma; Herth, Matthias M.; Jensen, Holger; Lindegren, Sture; Mikula, Hannes.
In: ChemPlusChem, Vol. 219, No. 84, 01.01.2019, p. 775-778.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
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
U2 - 10.1002/cplu.201900114
DO - 10.1002/cplu.201900114
M3 - Journal article
C2 - 31681526
AN - SCOPUS:85063866669
VL - 219
SP - 775
EP - 778
JO - ChemPlusChem
JF - ChemPlusChem
SN - 2192-6506
IS - 84
ER -
ID: 216920305