Mass Spectrometry-Based Kinetic & Site-Specific Profiling of Covalent Inhibitors Targeting VRK1

  • VRK1 is a synthetic lethality defined target in VRK2-low cancers
  • Presenting our strategy for inhibitor discovery that utilized a focused covalent library, intact protein MS, and cellular cysteine mapping
  • Demonstrating that mass spectrometry–based profiling can effectively identify covalent, isoform-selective inhibitors of VRK1