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Development of inhibitors for protein tyrosine kinases

Oncogene volume 19, pages 5690–5701 (2000)Cite this article

Abstract

In the last 5 years, through combinatorial chemistry, high-throughput screening, computational chemistry, and traditional medicinal chemistry, numerous inhibitors for various protein tyrosine kinases (PTKs) have been developed. The majority of these compounds are small molecules that compete at the ATP binding site of the catalytic domain of the enzymes. Some compounds such as pseudosubstrate-based peptide inhibitor binds to the peptide/protein substrate site of the catalytic domain. Some inhibitors, primarily monoclonal antibodies, bind to the extracellular domain of receptor tyrosine kinases. Some of these inhibitors are highly potent and selective. Several are currently undergoing clinical trials for a number of diseases such as cancer.

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Acknowledgements

This work was supported by NSF grant MCB9728399.

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  1. Selectide Corporation, A Subsidiary of Avantis., 1580 E. Hanely Blvd., Tucson, 85737, Arizona, AZ, USA

    Fahad A Al-Obeidi

  2. Division of Hematology/Oncology, and Department of Internal Medicine, UC Davis Cancer Center, University of California Davis, 4501 X Street, Sacramento, 95817, California, CA, USA

    Kit S Lam

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Al-Obeidi, F., Lam, K. Development of inhibitors for protein tyrosine kinases. Oncogene 19, 5690–5701 (2000). https://doi.org/10.1038/sj.onc.1203926

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