Abstract
Kinase inhibitors represent a relatively new class of drugs that offer novel therapies targeting specific malfunctioning kinase-mediated signaling pathways in oncology and potentially inflammation. As the ATP binding sites of the ∼500 human kinases are structurally conserved and because most current drugs target the ATP binding site, there is a need to profile all the kinases that a drug may bind and/or inhibit. We have developed a chemical proteomics method that affinity purifies kinases from cell or tissue lysates using kinase inhibitors immobilized on self-assembling monolayers. The method can be applied to assess the selectivity of a given kinase inhibitor and thus to guide its preclinical or clinical development.
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Acknowledgments
The authors thank Frank Weisbrodt for help with the figures and Gerard Drewes and Ulrich Kruse for helpful discussions.
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Bantscheff, M., Hobson, S., Kuster, B. (2012). Affinity Purification of Proteins Binding to Kinase Inhibitors Immobilized on Self-Assembling Monolayers. In: Kuster, B. (eds) Kinase Inhibitors. Methods in Molecular Biology, vol 795. Humana Press. https://doi.org/10.1007/978-1-61779-337-0_10
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DOI: https://doi.org/10.1007/978-1-61779-337-0_10
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