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Label-Free Fluorescent Kinase and Phosphatase Enzyme Assays with Supramolecular Host-Dye Pairs.
ChemistryOpen ( IF 2.5 ) Pub Date : 2019-11-12 , DOI: 10.1002/open.201900299
Yan-Cen Liu 1 , Shu Peng 1, 2 , Lora Angelova 1 , Werner M Nau 1 , Andreas Hennig 1
Affiliation  

The combination of the macrocyclic hosts p‐sulfonatocalix[4]arene and cucurbit[7]uril with the fluorescent dyes lucigenin and berberine affords two label‐free enzyme assays for the detection of kinase and phosphatase activity by fluorescence monitoring. In contrast to established assays, no substrate labeling is required. Since phosphorylation is one of the most important regulatory mechanisms in biological signal transduction, the assays should be useful for identification of inhibitors and activators in high‐throughput screening (HTS) format for drug discovery.

中文翻译:

使用超分子宿主染料对进行无标记荧光激酶和磷酸酶测定。

大环主体对基杯[4]芳烃和葫芦[7]脲与荧光染料光泽精和小檗碱的组合提供了两种无标记酶测定,用于通过荧光监测检测激酶和磷酸酶活性。与已建立的测定相反,不需要底物标记。由于磷酸化是生物信号转导中最重要的调节机制之一,因此这些检测应可用于以高通量筛选 (HTS) 形式识别抑制剂和激活剂以进行药物发现。
更新日期:2019-11-12
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