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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
MetabolomicsTargeting PI3K inhibitor resistance in breast cancer with metabolic drugs

Activating PIK3CA mutations, present in up to 40% of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (Her2-) breast cancer (BC) patients, can be effectively targeted with the alpha isoform-specific PI3K inhibitor Alpelisib. This treatment significantly improves ...

2026-08-21 | MTBLS11671 | MetaboLights
MetabolomicsDissection of two routes to naïve pluripotency using different kinase inhibitors
Embryonic stem cells (ESCs) can be maintained in the naïve state through inhibition of Mek1/2 and Gsk3 (2i). A relevant effect of 2i is the inhibition of Cdk8/19, which are negative regulators of the Mediator complex, responsible for the activity of enhancers. Inhibition of Cdk8/19 (Cdk8/19i) stimul...
2021-02-10 | MTBLS301 | MetaboLights
MetabolomicsThe Poly (ADP-Ribose) Polymerase inhibitor Veliparib and Radiation Cause Significant Cell Line Dependent Metabolic Changes in Breast Cancer Cells
Breast tumors are characterized into different subtypes based on their surface marker expression, which affects their prognosis and treatment. For example, triple negative breast cancer cells (ER-/PR-/Her2-) show reduced susceptibility towards radiotherapy and chemotherapeutic agents. Poly (ADP-ribo...
2016-11-07 | MTBLS337 | MetaboLights
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
ProteomicsKOPI - Kinase inhibitor proteome impact analysis
Kinase inhibitors often exhibit on/off-target effects, and efficient data analysis is essential for assessing these effects on the proteome. We developed a workflow for rapidly performing such a proteomic assessment, termed as kinase inhibitor proteome impact analysis (KOPI). We demonstrate KOPI’s ...
ORGANISM(S): Homo Sapiens (human) 
2022-06-16 | PXD029924 | JPOST Repository
ProteomicsProteomic profiling by array of tyrosine kinase activity in metastatic malignant melanoma from human tissue specimens
Tyrosine kinase activity profiling of metatstatic malignant melanoma and normal skin tissue samples was performed using peptide kinase arrays. All samples were run in triplicates with and withouth inhbitor PLX4032 and Sutent Malate in order to identify how tyrosine kinases responds to kinase inhibit...
ORGANISM(S): Homo sapiens 
2013-01-17 | E-MTAB-1245 | biostudies-arrayexpress
TranscriptomicsThe role of Raf-1 kinase inhibitor protein in the regulation of pancreatic beta cell proliferation in mice
AIMS/HYPOTHESIS: Manoeuvres aimed at increasing beta cell mass have been proposed as regenerative medicine strategies for diabetes treatment. Raf-1 kinase inhibitor protein 1 (RKIP1) is a common regulatory node of the mitogen-activated protein kinase (MAPK) and nuclear factor κB (NF-κB) pathways and...
ORGANISM(S): Mus musculus 
2012-11-19 | E-GEOD-31150 | biostudies-arrayexpress
TranscriptomicsTranscription profiling of human peripheral blood mononuclear cells treated with a CDK inhibitor
A genomics-based approach to identify pharmacodynamic biomarkers was used for a CDK (cyclin-dependent kinase) inhibitory drug. R547 is a potent CDK inhibitor with a potent anti-proliferative effect at pharmacologically relevant doses, and is currently in Phase I clinical trials. Utilizing preclinic...
ORGANISM(S): Homo sapiens 
2009-03-28 | E-GEOD-15389 | biostudies-arrayexpress
TranscriptomicsAT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity
Purpose: Deregulated phosphatidylinositol 3-kinase pathway signaling through AGC kinases including AKT, p70S6 kinase, PKA, SGK and Rho kinase, is a key driver of multiple cancers. The simultaneous inhibition of multiple AGC kinases may increase antitumor activity and minimize clinical resistance com...
ORGANISM(S): Homo sapiens 
2012-07-19 | E-GEOD-38008 | biostudies-arrayexpress
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