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MetabolomicsThe phosphofructo-2-kinase/fructose-2,6-bisphosphatase-3 inhibitor 3PO is a modulator of neutrophil metabolism, ROS production and NET release
Neutrophils are key effector leukocytes of the innate immune system and play a pivotal role in defending the host against microbial infections. Recent studies have identified a crucial link between glycolysis and neutrophil cellular functions. We have investigated in human neutrophils, the intricate...
2025-08-14 | MTBLS6215 | MetaboLights
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 
ProteomicsUse of a modified Multiplexed Inhibitor Bead assay to study kinome responses to cytostatic treatment in human cancer cell lines Triplicate Test: pilot study
In order to improve elution of proteins from the column, to reduce the cost as well as the hands on time of the analysis, we here present a modification of the Multiplexed Inhibitor Bead assay (MIB assay), where we elute the proteins from beads containing covalently bound inhibitors using trypsin di...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2017-03-29 | MSV000080744 | MassIVE
ProteomicsKinome Profiling of Primary Endometrial Tumors Using Multiplexed Inhibitor Beads and Mass Spectrometry Identifies SRPK1 As A Candidate Therapeutic Target
Protein kinases (collectively termed the kinome) represent one of the most tractable drug targets in the pursuit of new and effective cancer treatments. However, less than 20% of the kinome is currently being explored as primary targets for cancer therapy, leaving the majority of the kinome untarget...
ORGANISM(S): Homo sapiens (Human) 
2020-09-30 | PXD020357 | Pride
Endometrial Srpk1 
ProteomicsKinome Profiling of Gastrointestinal Stromal Tumors Using Multiplexed Inhibitor Beads and Mass Spectrometry Identifies Wee1 as a Candidate Therapeutic Target
Purpose: Management of gastrointestinal stromal tumor (GIST) has been revolutionized by the identification of activating mutations in KIT and PDGFRA and the clinical application of receptor tyrosine kinase (RTK) inhibitors in the advanced disease setting. Stratification of GIST into molecularly defi...
ORGANISM(S): Homo sapiens (Human) 
2021-09-09 | PXD020720 | Pride
Gastrointestinal stromal tumor Pdgfra Kit 
ProteomicsBead-based kinase phosphorylation profiling identifies SRC as a therapeutic target in glioblastoma
Here we describe a bead-based method capable of profiling tyrosine kinase phosphorylations in a multiplexed, high-throughput and low-cost manner. This approach allows for the discovery of tyrosine kinase-activating events, even when the DNA sequence is wild-type. In an effort to pilot the establishm...
ORGANISM(S): Homo sapiens 
2010-06-24 | E-GEOD-13808 | biostudies-arrayexpress
ProteomicsKinase Inhibitor Pulldown Assay (KiP) for Clinical Proteomics
Protein kinases are frequently dysregulated and/or mutated in cancer and represent essential targets for therapy. Accurate quantification is essential, but current approaches are inadequate. For breast cancer treatment for example, the identification and quantification of the protein kinase ERBB2 is...
ORGANISM(S): Homo sapiens (Human) 
2024-01-26 | PXD044655 | Pride
Human Breast Cancer Kinase 
ProteomicsDYRK3 protein-protein interactions in human cells
Quantitative affinity purification experiment was performed to identify the protein interactors of DYRK3 kinase in human cells. An additional pull-down experiment was carried out to study the changes of DYRK3 interactors with GSK-626616 kinase inhibitor treatment.
ORGANISM(S): Homo sapiens (Human) 
2018-07-05 | PXD007761 | Pride
Ap-ms Dyrk3 Silac Kinase inhibitor 
ProteomicsChemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors
Protein kinases are key components in signal transduction pathways and are established drug targets in oncology. Consequently, small molecule kinase inhibitors are on the rise but often show a rather broad target spectrum, potentially leading to toxic side effects. As a result, a broad assessment of...
ORGANISM(S): Homo sapiens (Human) 
2017-03-22 | PXD003373 | Pride
Kinase inhibitor Fech Photosensitivity Chemical proteomics Ferrochelatase Vemurafenib Kinobeads 
ProteomicsIn Cellulo Kinase Screen Identifies Novel MASTL Substrates
MASTL (microtubule-associated serine/threonine kinase-like) has emerged as a critical regulator of mitosis and as a potential oncogene in a variety of cancer types. To date, Arpp-19/ENSA are the only known substrates of MASTL. With the cellular roles of MASTL expanding and increased interest in deve...
ORGANISM(S): Homo sapiens (Human) 
2022-08-12 | PXD028678 | Pride
Akt Phospho-peptides Silac Agc kinase Kinase Mastl 
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