Sort   by:  
 Page size 
MetabolomicsFirst-in-class MKK4 inhibitors enhance liver regeneration and prevent liver failure

Diminished hepatocyte regeneration is a key feature of acute and chronic liver diseases and after extended liver resections, resulting in the inability to maintain or restore a sufficient functional liver mass. Therapies to restore hepatocyte regeneration are lacking, making liver transplantation...

2024-09-23 | MTBLS9434 | MetaboLights
MetabolomicsHypoxia Dependent Inhibition of Glioblastoma Cell Proliferation, Invasion, and Metabolism by the Choline-Kinase Inhibitor JAS239
Background: Elevated choline kinase alpha (ChoK) levels are observed in most solid tumors, including glioblastomas (GBM), and ChoK inhibitors have demonstrated limited efficacy in GBM models. Given that hypoxia is associated with resistance to GBM therapy, we hypothesized that tumor hypoxia c...
2024-06-18 | MTBLS6212 | MetaboLights
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 (ncbitaxon:9606) 
2018-01-12 | MSV000081932 | MassIVE
TranscriptomicsCharacterising the cellular activity of new Fibroblast Growth Factor Receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance.
Fibroblast growth factor receptors (FGFRs) can act as driving oncoproteins in certain cancers due to mutation, over-expression or activating gene fusions and are therefore attractive drug targets. Here we have characterized tumour cell responses to three new inhibitors of FGFR1-3, AZ12576089, AZ129...
ORGANISM(S): Homo sapiens 
2012-10-02 | E-TABM-1222 | biostudies-arrayexpress
TranscriptomicsAberrant ERK signaling causes resistance to EGFR kinase inhibitors
The clinical efficacy of EGFR kinase inhibitors is limited by the development of drug resistance. The irreversible EGFR kinase inhibitor WZ4002 is effective against the most common mechanism of drug resistance mediated by the EGFR T790M mutation. Here we show that in multiple complementary models ha...
ORGANISM(S): Homo sapiens 
2012-10-01 | E-GEOD-37699 | biostudies-arrayexpress
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 
ProteomicsEffect of Kinase Inhibitors on Intraerythrocytic Plasmodium falciparum Phosphoproteome
Three flasks of asynchronous blood stage P. falciparum Dd2 culture were grown to ~15% parasitemia, 4% hematocrit using the Trager- Jensen method. Per biological replicate, parasites were treated with 5 x EC50 or EC90 of compound depending on the slope of the EC50 curve for 3 hours. Compounds are DC-...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) Plasmodium Falciparum Dd2 (ncbitaxon:57267) 
2023-04-03 | MSV000091619 | MassIVE
MetabolomicsRBC Balanced Immuno-inflammatory Signatures Identify Advanced Breast Cancer Patients on CDK4/6 Inhibitors at Increased Risk of Progression and Death

Recent studies show red blood cell (RBC) plays an essential role in regulating immunity. Nevertheless, the association of immuno-inflammatory parameters, especially RBC balanced signatures, with survival outcomes and adverse events still require investigation for advanced breast cancer (ABC) pati...

2025-04-15 | MTBLS10792 | MetaboLights
ProteomicsIlluminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics
Kinase inhibitors (KIs) are important cancer drugs but often display polypharmacology that is molecularly not understood. This disconnect is particularly apparent in cancer entities such as sarcomas for which the oncogenic drivers are often not clear. To investigate more systematically how the cellu...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2023-01-11 | MSV000091043 | MassIVE
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 
Sort   by:  
 Page size