Application of new assay technologies to shed light on kinase drug discovery.
The human kinome comprises 518 known protein kinases and more than 20 lipid kinases. Nearly all aspects of control within a cell are modulated by reversible phosphorylation of proteins, mediated by protein kinases.
Abnormal phosphorylation is a cause or effect of many diseases including cancer and inflammatory diseases, hence many pharma and biotech companies continue to undertake research and development in this area believing it to be of clinical importance. While we can congratulate ourselves on our success in identifying more than 37 kinase inhibitor compounds that have made it to patients and more than 250 drug candidates that are undergoing clinical evaluation, arguably we have only scratched the surface of kinase biology. A seminal paper1 published in Science in December 2017 provides an interesting insight into drug discovery within the kinome space and, to use the space analogy, helps us to realise that at best we have only explored our own kinase solar system, let alone our galaxy and what lies beyond in kinome space...
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