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Label-Free Fluorescent Kinase and Phosphatase Enzyme Assays with Supramolecular Host-Dye Pairs |
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| Authors: | Yan-Cen Liu Dr Shu Peng Lora Angelova Prof Dr Werner M Nau Dr Andreas Hennig |
| Institution: | 1. Department of Life Sciences and Chemistry, Jacobs University Bremen gGmbH, Campus Ring 1, 28759 Bremen, Germany;2. Department of Life Sciences and Chemistry, Jacobs University Bremen gGmbH, Campus Ring 1, 28759 Bremen, Germany
College of Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Key Laboratory of Functional Polymer Materials, Ministry of Education, Nankai University, Tianjin, 300071 Tianjin China |
| Abstract: | The combination of the macrocyclic hosts p-sulfonatocalix4]arene and cucurbit7]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. |
| Keywords: | fluorescence enzyme assay host-guest chemistry kinase phosphatase |