Multifunctional Clickable Reagents for Rapid Bioorthogonal Astatination and Radio-Crosslinking.
Chempluschem
; 84(7): 775-778, 2019 07.
Article
em En
| MEDLINE
| ID: mdl-31681526
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 inâ
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.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos Radiofarmacêuticos
/
Química Click
Limite:
Humans
Idioma:
En
Revista:
Chempluschem
Ano de publicação:
2019
Tipo de documento:
Article