期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 59, 期 8, 页码 3272-3279出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201913314
关键词
bioorthogonal reactions; enzyme activity imaging; fluorescent probes; nanoparticles; self-assembly
资金
- Stanford Cancer Translational Nanotechnology Training grant - National Cancer Institute (NCI) [T32CA196585]
- NCI, Stanford CCNE-TD [U54CA199075]
- Stanford Bio-X Interdisciplinary Initiatives Seed Grants Program (IIP) award
The condensation reaction between 6-hydroxy-2-cyanobenzothiazole (CBT) and cysteine has been shown for various applications such as site-specific protein labelling and in vivo cancer imaging. This report further expands the substrate scope of this reaction by varying the substituents on aromatic nitriles and amino thiols and testing their reactivity and ability to form nanoparticles for cell imaging. The structure-activity relationship study leads to the identification of the minimum structural requirement for the macrocyclization and assembly process in forming nanoparticles. One of the scaffolds made of 2-pyrimidinecarbonitrile and cysteine joined by a benzyl linker was applied to design fluorescent probes for imaging caspase-3/7 and beta-galactosidase activity in live cells. These results demonstrate the generality of this system for imaging hydrolytic enzymes.
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