Establishing an activity-based protein profiling platform to screen in situ kinase inhibitor engagement

ABSTRACT: Activity-based protein profiling is a powerful tool to study target engagement in complex biological environments. XO44 is a chemical probe based on the scaffold of a promiscuous kinase binder, which covalently reacts with a conserved lysine in the ATP-binding pocket of kinases. Pretreatment of cells with a drug (candidate) results in competition of XO44 binding, which can be interpreted as in situ target engagement. Here, a workflow is presented which is optimized for kinome coverage, reproducibility and data processing. This dataset pertains to the selectivity testing of Midostaurin in MV4-11 cells. (Phosphoproteomics)

INSTRUMENT(S):

ORGANISM(S): Homo Sapiens (human)

SUBMITTER: Berend Gagestein  

LAB HEAD: Mario van der Stelt

PROVIDER: PXD055387 | Pride | 2025-04-09

REPOSITORIES: Pride