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Next Generation CSox-based Substrate Sensors for Continuous, Homogeneous and Quantitative Monitoring of Protein Kinase ActivityDownload
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February 13, 2017
There are 518 human protein kinases, many of which have been shown to be dysregulated in disease states and therefore comprise greater than 30% of all drug development. Harnessing chelation-enhanced fluorescence (CHEF) with the sulfonamido-oxine (Sox) chromophore in peptide or protein substrates has created a simple yet powerful method to measure the activity of protein kinases using a direct, single-step homogeneous, fluorescence-based assay for rapid and sensitive detection of serine/threonine and tyrosine kinase activities in a continuous (kinetic) format with both recombinant enzymes and with crude cell or tissue lysates. This platform is ideal for elucidation of drug mechanism of action and is increasingly being applied earlier in the drug development process to address challenges and opportunities for next generation kinase inhibitors. Here we demonstrate the use of high-throughput peptide synthesis for degenerate Sox-based libraries to systematically identify improved substrates. Application of this approach to create robust assays for studying kinase activity and kinase inhibitor screening or characterization is presented.
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