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MetabolomicsMicrobiome Metabolism of Dietary Phytochemicals Controls the Anticancer Activity of PI3K Inhibitors
Phosphatidylinositol 3-kinase (PI3K) signaling is both the effector pathway of insulin and among the most frequently activated pathways in human cancer. In murine cancer models, the efficacy of PI3K inhibitors is dramatically enhanced by a ketogenic diet, with a proposed mechanism involving dietary ...
2025-03-26 | MTBLS10944 | MetaboLights
TranscriptomicsGene expression profiling upon PI3K inhibition using different inhibitors
Activation of the phosphoinositide 3-kinase (PI3K)/Akt signaling pathway is one the most frequent genetic events in human cancer. Therefore, the development of PI3K inhibitors has attracted much attention. We previously described the pyrazolopyrimidine derivative ETP-45658 as a potent inhibitor of P...
ORGANISM(S): Homo sapiens 
2014-04-08 | E-GEOD-56579 | biostudies-arrayexpress
TranscriptomicsResistance to PI3K/mTOR inhibitor PF-04691502 in KRAS mutant colorectal cancer models reveals a sensitivity to combination with EGFR inhibition
We explored potential bypass mechanisms to PI3K/mTOR-directed therapy in KRAS mutant CRC models, utilizing genetically engineered mouse models (GEMM) to generate acquired resistance to the targeted dual PI3K/mTOR small molecule inhibitor PF-04691502. Transcriptomic analysis revealed a dynamic stem-l...
ORGANISM(S): Mus musculus 
2014-08-31 | E-MTAB-2510 | biostudies-arrayexpress
ProteomicsMass spectrometry-based proteomics reveals potential roles of NEK9 and MAP2K4 in resistance to PI3K inhibitors in triple negative breast cancer

Filip Mundt, Sandeep Rajput, Shunqiang Li, Kelly Ruggles, Arshag D. Mooradian, Philipp Mertins, Michael A. Gillette, Karsten Krug, et al., Cancer Res. 2018 May 15;78(10):2732-2746. doi: 10.1158/0008-5472.CAN-17-1990.

Activation of phosphoinositide 3-kinase (PI3K) signaling is frequently obs...

ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2018-10-19 | MSV000083050 | MassIVE
TranscriptomicsComparative study of a mTOR inhibitor, a pan-PI3K inhibitor and a dual PI3K/mTOR inhibitor in MCL
Phosphatidylinositol-3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) pathway activation contributes to mantle cell lymphoma (MCL) pathogenesis and drug resistance. However, the use of mTOR inhibitors as single agents have shown limited clinical efficacy in relation with drug activation of f...
ORGANISM(S): Homo sapiens 
2013-12-14 | E-GEOD-53309 | biostudies-arrayexpress
TranscriptomicsTargeting resistance to Smoothened antagonists by inhibiting the PI3K pathway
Mutations in Hedgehog (Hh) pathway genes, leading to constitutive activation of Smoothened (Smo), occur in sporadic medulloblastoma, the most common brain cancer in children. Antagonists of Smo induce tumor regression in mouse models of medulloblastoma and hold great promise for targeted therapy fo...
ORGANISM(S): Mus musculus 
2010-09-29 | E-GEOD-19657 | biostudies-arrayexpress
TranscriptomicsTranscription profiling by array of human prostate cancer cells enriched for cell surface markers CD44/CD133/alpha 2 beta 1 integrin
Self-renewing tumor initiating cells that are capable of differentiation and responsible for tumor growth have been isolated from cancers and cell lines. If such minor populations are associated with tumor progression, understanding molecular pathways that are required for viability and maintenance ...
ORGANISM(S): Homo sapiens 
2009-01-13 | E-GEOD-10832 | biostudies-arrayexpress
TranscriptomicsComparison of gene expression alterations induced by distinct PI3K inhibitors
The goal is the characterization of the off-target activity of BKM120 observed in A2058 human melanoma cell line at IC90 concentration (3.606 µM) but not at lower concentrations. Controls are BEZ235, GDC0941, showing no off-target activity. A secondary objective is the characterizations of drug eff...
ORGANISM(S): Homo sapiens 
2012-06-30 | E-GEOD-33643 | biostudies-arrayexpress
TranscriptomicsCombined PI3K/mTOR and MEK Inhibition Provides Broad Anti-Tumor Activity in Faithful Murine Cancer Models
Anticancer drug development is an inefficient process, with potential therapeutics demonstrating a high attrition rate due to lack of efficacy in Phase II/III testing. In an effort to develop improved pre-clinical predictors of efficacy, we and others have turned to testing in genetically engineere...
ORGANISM(S): Mus musculus 
2012-08-21 | E-GEOD-35722 | biostudies-arrayexpress
ProteomicsN-acetylcysteine overcomes NF1-loss driven resistance to PI3K alpha inhibition in breast cancer.
Breast cancer is the second most common cancer type worldwide, representing 25% of all cancers in women. PIK3CA is one of the most frequently mutated genes in breast cancer and mutations result in constitutive activation of the PI3K/mTOR pathway. More than 30 inhibitors against PI3K/mTOR are being t...
ORGANISM(S): Homo sapiens (Human) 
2023-03-30 | PXD034644 | Pride
Tmt Pi3k alpha inhibition Phospho proteomics Breast cancer 
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