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Targeting protein kinases

Nature Reviews Drug Discovery volume 3, pages 993–994 (2004)Cite this article

Protein kinases are considered to be the second most important group of drug targets after G-protein-coupled receptors1,2. Aberrant kinase activity is implicated in a variety of human diseases, in particular those involving inflammatory or proliferative responses, such as cancer, rheumatoid arthritis, cardiovascular and neurological disorders, asthma and psoriasis. Directly or indirectly, more than 400 human diseases have been connected to protein kinases. The ability to modulate kinase activity therefore represents an attractive therapeutic strategy for the treatment of human illnesses. However, despite the wealth of potential targets, the most advanced compounds currently on the market or in clinical development target only a handful of the best-characterized kinases.

The modulation of kinase activity can be achieved through several strategies: inhibition of phosphorylation activity by blocking ATP binding; disruption of protein–protein interactions; and downregulation of kinase gene expression by antisense or RNA interference approaches.

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Figure 1: Actual and projected sales for currently marketed oncology protein kinase inhibitors.

References

  1. Vlahovic, G. et al. Activation of tyrosine kinases in cancer. The Oncologist 8, 531–538 (2003).

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  2. Cohen, P. Protein kinases, the major drug targets of the 21st century? Nature Rev. Drug Discov. 1, 309–316 (2002).

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Authors and Affiliations

  1. Ph.D., is a Senior Research Analyst at Life Science Insights, 5 Speen Street, Framingham, 01701, Massachusetts, USA

    Irena Melnikova

  2. Ph.D., is VP of Research at Life Science Insights, 5 Speen Street, Framingham, 01701, Massachusetts, USA

    James Golden

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  1. Irena Melnikova
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  2. James Golden
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The Pharmaceutical Research and Manufacturers of America

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Melnikova, I., Golden, J. Targeting protein kinases. Nat Rev Drug Discov 3, 993–994 (2004). https://doi.org/10.1038/nrd1600

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