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ProteomicsKinome-profiling enabled discovery of a LATS1/2 inhibitor with wound healing potential
System-level mapping of kinase inhibitors polypharmacology can uncover opportunities for drug repurposing and identify starting points for medicinal chemistry campaigns aimed at novel targets. Here, we describe a large-scale profiling of 257 kinase inhibitors that revealed domains of promiscuity, po...
ORGANISM(S): Homo sapiens (Human) 
2026-07-15 | PXD073488 | Pride
Human Proteomics Kinase selectivity profiling Kinase inhibitor 
ProteomicsTarget Landscape of Clinical Kinase Inhibitors
Here, we provide a comprehensive overview of the selectivity profiles of 242 kinase inhibitors currently in clinical trials. We screened available inhibitors against human protein kinases by using the Kinobead technology resulting in a drug matrix identifying the druggable kinome and related protein...
ORGANISM(S): Homo sapiens (Human) 
2017-12-01 | PXD005336 | Pride
Target Mass spectrometry Chemical proteomics Kinase inhibitors Clinical kinase inhibitors Selectivity Lc-ms/ms 
ProteomicsDetermining MELK inhibitor specificity using MIB/MS
The key objectives of this study were to evaluate the selectivity profiles of three MELK inhibitors, 8a, HTH, and OTS, using a cell-based assay, in order to identify a highly selective inhibitor to subsequently investigate MELK function. To this end, we utilized a chemical proteomics approach called...
ORGANISM(S): Homo sapiens (Human) 
2020-01-09 | PXD016022 | Pride
Chemoproteomics Lfq Kinase enrichment 
UnknownTargeted kinase selectivity from kinase profiling data.
Not available
S-EPMC4025760 | biostudies-literature
ProteomicsChemoproteomic selectivity profiling of PIKK and PI3K kinase inhibitors
"Here, we report the development of a novel version of Kinobeads that extends kinome coverage to PIKK and PI3K kinases. This is achieved by inclusion of two affinity probes derived from the clinical PI3K/MTOR inhibitors Omipalisib and BGT226. The new affinity matrix was used to profile 13 clinical a...
ORGANISM(S): Homo sapiens (Human) 
2019-03-29 | PXD011719 | Pride
Chemoproteomics" "kinobeads Drug profiling 
ProteomicsDiscovery of dedicated EPHA2 inhibitors - Medicinal chemistry meets chemical proteomics
The receptor tyrosine kinase EPHA2 has gained interest as therapeutical drug target in cancer and infectious diseases in the past years. However, EPHA2 research and EPHA2 based therapies have been hampered by the lack of selective small molecule EPHA2 inhibitors. We report on the synthesis and evalu...
ORGANISM(S): Homo sapiens (Human) 
2017-05-30 | PXD006193 | Pride
Eph receptor Drug discovery Selectivity profiling Inhibitors Chemical proteomics 
ProteomicsDefining the landscape of EPHA2 Inhibition by Clinical Kinase Inhibitors
The receptor tyrosine kinase EPHA2 plays important roles in oncogenesis, metastasis and treatment resistance but therapeutic targeting, drug discovery or investigation of EPHA2 biology is hampered by the lack of appropriate inhibitors and structural information on how these interact with the protein...
ORGANISM(S): Homo sapiens (Human) 
2016-12-23 | PXD004112 | Pride
Epha2 co-crystals Selectivity profiling Chemical proteomics Residue categorization Drug protein interactions 
ProteomicsSingle methyl group positioning opens new chemical space for EPH receptor kinase inhibition
EPHrin receptors (EPH) are transmembrane receptor tyrosine kinases. Their extracellular domains bind specifically to ephrin A/B ligands, and this binding modulates the intracellular kinase activity. EPHs are key players in bidirectional intercellular signalling, controlling cell morphology, adhesion...
ORGANISM(S): Homo sapiens (Human) 
2018-09-05 | PXD009188 | Pride
Eph receptor Selectivity profiling Kinase inhibitor Kinobeads 
ProteomicsEvaluation of of kinase acitivity profiling using chemical proteomics
Evaluation of kinase binding to immobilized inhibitors upon kinase activation. Comparison of cheomproteomic binding changes to phosphoproteomic activation profiles.
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2016-10-21 | MSV000080272 | MassIVE
ProteomicsPRM-LIVE with Trapped Ion Mobility Spectrometry and Its Application in Selectivity Profiling of Kinase Inhibitors
Raw data files for the manuscript "PRM-LIVE with Trapped Ion Mobility Spectrometry and Its Application in Selectivity Profiling of Kinase Inhibitors"
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2021-06-02 | MSV000087561 | MassIVE
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