期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 15, 期 12, 页码 2575-2584出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c7ob00370f
关键词
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资金
- Institut Universitaire de France (IUF)
- Burgundy region
We report a reaction-based strategy for the fluorogenic detection of protease activity. Based on the covalent-assembly probe design principle recently put forward by the Yang group for detection of Sarin related threats (J. Am. Chem. Soc., 2014, 136, 6594-6597), we have designed two unusual nonfluorescent caged precursors (mixed bis-aryl ethers) which are readily converted into a fluorescent unsymmetrical pyronin dye through a domino cyclisation-aromatisation reaction triggered by penicillin G acylase (PGA) or leucine aminopeptidase (LAP). Fluorescence-based in vitro assays and HPLCfluorescence/- MS analyses support the claimed activation mechanism whose the further implementation to smart imaging agents for the study of protease function in vivo is expected.
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