- 标题
- 摘要
- 关键词
- 实验方案
- 产品
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Identification of Potent Caspase-8 Inhibitors from a Library of Fluorescent Natural Products Screened by an AIEgen-based Light-up Probe
摘要： Fluorescent natural products are a rich source of drugs and chemical probes. But their inborn fluorescence may interfere with the fluorescence-based screening assays. Caspase-8 is a key player in apoptosis. Inhibition of caspase-8 found to be beneficial for inflammatory and neurodegenerative diseases. But its small molecular inhibitors remain sparsely reported. In this study, we firstly developed a caspase-8 targeting light-up probe based on an AIEgen. This fluorescent dye has a Stokes shift of 200 nm which could avoid the inborn fluorescence signal of natural products. When screening a library of 86 fluorescent natural products, we found for the first time Gossypol showed potent inhibition towards caspase-8 in vitro and in situ. This unique kind of light-up probe coupled with colored natural products could be an efficient way in the hit discovery for druggable targets.
关键词： natural product,aggregation-induced emission,inhibitor screening,caspase-8,fluorescence
更新于2025-09-23 15:22:29
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A carbapenem-based fluorescence assay for the screening of metallo-β-lactamase inhibitors
摘要： Reported herein is a fluorescence assay for the rapid screening of metallo-β-lactamase (MBL) inhibitors. This assay employs a fluorogenic carbapenem CPC-1 as substrate and is compatible with all MBLs, including B1, B2 and B3 subclass MBLs. The efficiency of this assay was demonstrated by the rapid inhibition screening of a number of molecules against B2 MBL CphA and 2,3-dimercaprol was identified as a potent CphA inhibitor.
关键词： Fluorescence,Inhibitor,Screening assay,Metallo-β-lactamase
更新于2025-09-10 09:29:36