Protein kinases are a diverse group of 518 enzymes whose dysregulation underlies 400 or more human diseases across therapeutic areas and especially oncology and inflammation. Currently, 30% of all drug development efforts are focused on protein kinases. Although many drugs are approved or in clinical trials, these are predominately ATP-competitive inhibitors. More recently, there has been a surge in the generation of kinase inhibitors with different modes of action, where new tools are needed to effectively characterize inhibitor function, predict drug potency and to drive decisions earlier in the drug development process.
PhosphoSens® Cys-Sox-based sensors harness chelation-enhanced fluorescence by integrating the sulfonamido-oxine (Sox) chromophore to create optimized peptide sensors for the quantitative and homogenous detection of kinase and phosphatase activity. The same sensor can be used for kinetic or endpoint assay formats using the CLARIOstar Plus microplate reader.
