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Overview of Current Type I/II Kinase Inhibitors

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Next Generation Kinase Inhibitors

Abstract

Research on kinase-targeting drugs has made great strides over the last 30 years and is attracting greater attention for the treatment of yet more kinase-related diseases. Currently, 42 kinase drugs have been approved by the FDA, most of which (Wilson et al., Cancer Research 78(1):15–29, 2018) are Type I/II inhibitors. Notwithstanding these advances, it is desirable to target additional kinases for drug development as more than 200 diseases, particularly cancers, are directly associated with aberrant kinase regulation and signaling. Here, we review the extant Type I/II drugs systematically to obtain insights into the binding pocket characteristics, the associated features of Type I/II drugs, and the mechanism of action to facilitate future kinase drug design and discovery. We conclude by summarizing the main successes and limitations of targeting kinases for the development of drugs.

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Acknowledgments

Thanks to Peng Wu for useful insights and corrections when reviewing this manuscript.

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Authors and Affiliations

  1. Department of Biomedical Engineering, University of Virginia, Charlottesville, VA, USA

    Zheng Zhao & Philip E. Bourne

  2. Data Science Institute, University of Virginia, Charlottesville, VA, USA

    Philip E. Bourne

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  1. Zheng Zhao
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Correspondence to Philip E. Bourne .

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  1. Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, USA

    Paul Shapiro

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Zhao, Z., Bourne, P.E. (2020). Overview of Current Type I/II Kinase Inhibitors. In: Shapiro, P. (eds) Next Generation Kinase Inhibitors. Springer, Cham. https://doi.org/10.1007/978-3-030-48283-1_2

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