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Fragment-Based Design of Kinase Inhibitors: A Practical Guide

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Book cover Fragment-Based Methods in Drug Discovery

Part of the book series: Methods in Molecular Biology ((MIMB,volume 1289))

Abstract

Fragment-based drug design has become an important strategy for drug design and development over the last decade. It has been used with particular success in the development of kinase inhibitors, which are one of the most widely explored classes of drug targets today. The application of fragment-based methods to discovering and optimizing kinase inhibitors can be a complicated and daunting task; however, a general process has emerged that has been highly fruitful. Here a practical outline of the fragment process used in kinase inhibitor design and development is laid out with specific examples. A guide to the overall process from initial discovery through fragment screening, including the difficulties in detection, to the computational methods available for use in optimization of the discovered fragments is reported.

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Acknowledgement

The author is indebted to Drs. M. Vieth, J. Sutherland, J. Toth, D. Robertson, and C. Humblet for valuable suggestions and support of this chapter.

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  1. Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN, 46285, USA

    Jon A. Erickson

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Correspondence to Jon A. Erickson .

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  1. Pennsylvania Drug Discovery Institute, Doylestown, Pennsylvania, USA

    Anthony E. Klon

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Erickson, J.A. (2015). Fragment-Based Design of Kinase Inhibitors: A Practical Guide. In: Klon, A. (eds) Fragment-Based Methods in Drug Discovery. Methods in Molecular Biology, vol 1289. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-2486-8_13

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  • DOI: https://doi.org/10.1007/978-1-4939-2486-8_13

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