Articles | Volume 3, issue 1
Research article
20 May 2022
Research article |  | 20 May 2022

Imatinib disassembles the regulatory core of Abelson kinase by binding to its ATP site and not by binding to its myristoyl pocket

Stephan Grzesiek, Johannes Paladini, Judith Habazettl, and Rajesh Sonti

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Field: Liquid-state NMR | Topic: Applications – biological macromolecules
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Short summary
We show here that binding of the anticancer drug imatinib to the ATP site of Abelson kinase and not binding to its allosteric site coincides with the opening of the kinase regulatory core at nanomolar concentrations. This has implications for the understanding of Abelson’s kinase regulation and activity during medication as well as for the design of new Abelson kinase inhibitors.