Proteomics

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Differential kinobeads selectivity profiling

ABSTRACT: The goal of this project was to use differential kinobeads profiling for the discrimination of reversible and irreversible kinase targets of different covalent kinase inhibitors. For this, differences in target engagement measured in a lysate- and a cell-based kinobeads assay were compared in a kinome-wide scale.

INSTRUMENT(S): Orbitrap Fusion Lumos, Q Exactive

ORGANISM(S): Homo Sapiens (human)

TISSUE(S): Epithelial Cell Of Alveolus Of Lung, B Cell

SUBMITTER: Maria Faelth Savitski  

LAB HEAD: Marcus Bantscheff

PROVIDER: PXD007920 | Pride | 2017-10-13

REPOSITORIES: Pride

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Publications

Differential Kinobeads Profiling for Target Identification of Irreversible Kinase Inhibitors.

Dittus Lars L   Werner Thilo T   Muelbaier Marcel M   Bantscheff Marcus M  

ACS chemical biology 20170912 10

Chemoproteomics profiling of kinase inhibitors with kinobeads enables the assessment of inhibitor potency and selectivity for endogenously expressed protein kinases in cell lines and tissues. Using a small panel of targeted covalent inhibitors, we demonstrate the importance of measuring covalent target binding in live cells. We present a differential kinobeads profiling strategy for covalent kinase inhibitors where a compound is added either to live cells or to a cell extract that enables the co  ...[more]

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