Articles | Volume 3, issue 1
https://doi.org/10.5194/mr-3-91-2022
https://doi.org/10.5194/mr-3-91-2022
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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Interactive discussion

Status: closed

Comment types: AC – author | RC – referee | CC – community | EC – editor | CEC – chief editor | : Report abuse
  • RC1: 'Comment on mr-2022-6', Anonymous Referee #1, 29 Mar 2022
  • RC2: 'Comment on mr-2022-6', Anonymous Referee #1, 03 Apr 2022
  • RC3: 'Comment on mr-2022-6', Paul Schanda, 04 Apr 2022
  • CC1: 'Comment on mr-2022-6', Oliver Hantschel, 21 Apr 2022
  • CEC1: 'Comment on mr-2022-6', Gottfried Otting, 22 Apr 2022
    • AC1: 'Reply on CEC1', Stephan Grzesiek, 24 Apr 2022
  • CC2: 'Comment on mr-2022-6', Dorothee Kern, 24 Apr 2022
    • RC4: 'Reply on CC2', Paul Schanda, 24 Apr 2022
    • CC3: 'Reply on CC2', Dorothee Kern, 24 Apr 2022
    • CC4: 'Reply on CC2', Dorothee Kern, 24 Apr 2022
  • RC5: 'Comment on mr-2022-6', Anonymous Referee #3, 24 Apr 2022
  • EC1: 'Comment on mr-2022-6', Geoffrey Bodenhausen, 01 May 2022

Peer review completion

AR: Author's response | RR: Referee report | ED: Editor decision
AR by Stephan Grzesiek on behalf of the Authors (08 May 2022)  Author's response    Author's tracked changes    Manuscript
ED: Publish as is (10 May 2022) by Geoffrey Bodenhausen
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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.