CHAPTER 2: New Screening Approaches for Kinases
Published:31 Oct 2018
D. H. Drewry, B. W. King, C. I. Wells, and W. J. Zuercher, in Kinase Drug Discovery: Modern Approaches, ed. R. A. Ward and F. W. Goldberg, The Royal Society of Chemistry, 2018, pp. 9-33.
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Kinases are important targets for drug discovery as evidenced by the US FDA approval of over 30 small molecule kinase inhibitors over the last two decades. A wide range of assay technologies have been utilized to quantify inhibitor activity or binding and to assess inhibitor selectivity across the kinome. In this chapter we review some of the modern and perhaps non-traditional methods being used in academic and industrial laboratories, including fragment based approaches DNA encoded library technology (ELT), differential scanning fluorimetry (DSF), chemical proteomics and cellular screening. We highlight the potential advantages offered by each of these methods, along with some of the potential issues and provide illustrative examples.