Kinase Screening: The Path Forward
Gordon Alton, President and CEO Altonyx Consulting
Protein kinases represent one of the largest groups of drug targets due to their critical involvement in important pathophysiological pathways. More than 600 kinase inhibitors are now in development. Multiple biopharmaceutical companies perform high-throughput screening (HTS) for many different kinases each year. Given the large number of screens run, there has been a corresponding increase in the commercial reagent and service industries for kinase assays, kits, proteins and kinomic selectivity profiling services. Currently, the challenge for scientists initiating kinase HTS is to adequately characterize the advantages and disadvantages of the different assay technologies. There are now more than 30 distinct assays that are commercially available. However, some assay systems are becoming more popular to use. These include time-resolved fluorescent resonance energy transfer, coupled enzyme assays, and various bead-based assays. In the past the per-well cost of the assay was critical with most groups aiming for less than 10 cents per well. This is not as critical today because it is widely recognized that screening a focused kinase inhibitor library (KIL) rather than a broad "full file" of inhibitors provides sufficient numbers of hits to power a lead identification campaign. Several companies supply quality KILs that can bestow a reasonable foundation to initiate HTS.
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