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Biological & Disease Relevance


Kinase Biological and Disease Relevance Current research shows that precise targeting of specific aspects of kinase cascades can provide previously unattainable breakthroughs for disease therapies.

The importance of the protein kinase family is underscored by the numerous disease states that arise due to disregulation of kinase activity. Today, with more than 500 protein kinases identified in the human genome, research has focused on understanding the molecular details of the roles kinases play in regulating critical cellular activities.

Aberrant cell signaling by many of these protein kinases can lead to diseases, such as cancer, Alzheimer's disease, and type II diabetes. Inhibitors that target protein kinases have proven efficacious as novel therapeutics; hence, their continued development is the current focus of many drug discovery groups.

  • Click to view list of kinase targets

    Newest kinase targets and their disease relevance:
    Met
    Clinically relevant mutations of Met: D1246H, D1246N, Y1248C, Y1248D, Y1248H & M1268T
    The product of the met proto-oncogene (Met) is a tyrosine kinase receptor for hepatocyte growth factor (HGF). Receptor activation triggers a unique process of differentiation that involves the promotion of cell growth, protection from apoptosis, control of cell dissociation, and migration into extracellular matrices. Deregulation of Met activity is common in human cancers and is associated with poor outcome. The residue substitutions described above are mutations in the Met kinase domain that have been identified in patients with papillary renal carcinomas. In vitro studies on mutated versions of Met have demonstrated constitutive phosphorylation of the receptors, downstream pathway activation and cell motility that is consistent with the oncogenic nature of these mutations.





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