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ProteomicsNovel Eph receptor tyrosine kinase inhibitors block colorectal cancer cell growth
Despite advances, treatment of unresectable colorectal cancer remains a clinical challenge and the incidence of this malignancy is increasing in individuals below the age of fifty. Integrated genomic, transcriptomic, proteomic, and mechanistic studies identified the tyrosine kinase receptors EphB2 a...
ORGANISM(S): Homo sapiens (Human) 
2024-05-23 | PXD031880 | Pride
Affinity pulldowns Kinobeads Lc-ms/ms 
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 
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 
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 
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 
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 
ProteomicsPLK1 phosphorylation of Epstein-Barr virus nuclear antigen 2
The Epstein-Barr virus nuclear antigen 2 (EBNA2) initiates and maintains the proliferation of infected B cells. In search of additional cellular strategies, that control EBNA2 function, we have performed a label-free mass spectrometry-based quantification of cellular proteins in EBNA2 immuno-precipi...
ORGANISM(S): Human herpesvirus 4 strain B95-8 
2021-08-22 | PXD022970 | Pride
Cancer Phosphoproteomics Mass spectrometry 
ProteomicsGlobal Proteome Analysis of the NCI-60 Cell Line Panel
The NCI-60 cell line collection is a very widely used panel for the study of cellular mechanisms of cancer in general and in vitro drug action in particular. It is a model system for the tissue types and genetic diversity of human cancers and has been extensively molecularly characterized. Here, we ...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2018-03-23 | MSV000082204 | MassIVE
ProteomicsGlobal Proteome Analysis of the NCI-60 Cell Line Panel, part 2
The NCI-60 cell line collection is a very widely used panel for the study of cellular mechanisms of cancer in general and in vitro drug action in particular. It is a model system for the tissue types and genetic diversity of human cancers and has been extensively molecularly characterized. Here, we ...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2018-03-23 | MSV000082203 | MassIVE
ProteomicsGlobal Proteome Analysis of the NCI-60 Cell Line Panel, part 3
The NCI-60 cell line collection is a very widely used panel for the study of cellular mechanisms of cancer in general and in vitro drug action in particular. It is a model system for the tissue types and genetic diversity of human cancers and has been extensively molecularly characterized. Here, we ...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2018-03-23 | MSV000082205 | MassIVE
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