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

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

doi:https://doi.org/10.5194/mr-3-91-2022

Articles | Volume 3, issue 1

https://doi.org/10.5194/mr-3-91-2022

© Author(s) 2022. This work is distributed under
the Creative Commons Attribution 4.0 License.

https://doi.org/10.5194/mr-3-91-2022

© Author(s) 2022. This work is distributed under
the Creative Commons Attribution 4.0 License.

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

Supplement

https://doi.org/10.5194/mr-3-91-2022-supplement

Data sets

Imatinib disassembles the regulatory core of Abelson kinase by binding to its ATP site and not by binding to its myristoyl pocket S. Grzesiek, J. Paladini, J. Habazettl, and R. Sonti https://doi.org/10.5281/zenodo.6368036

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.