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ProteomicsEvaluation of phospho-tyrosine antibodies for label-free phosphoproteomics
In the past decade multiple tyrosine kinase inhibitors (TKIs) have been implemented in standard treatment regimens for patients with cancer. Unfortunately the majority of patients develops resistance to these drugs. Reliable tools for analysis of pharmacodynamic effects and drug resistance mechanism...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2016-10-21 | MSV000080270 | 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
ModelsBouchnita2019 - A multiscale model to design therapeutic strategies that overcome drug resistance to tyrosine kinase inhibitors in multiple myeloma
Drug resistance (DR) is a phenomenon characterized by the tolerance of a disease to pharmaceutical treatment. In cancer patients, DR is one of the main challenges that limit the therapeutic potential of the existing treatments. Therefore, overcoming DR by restoring the sensitivity of cancer cells wo...
2020-01-09 | MODEL1912170004 | BioModels
TranscriptomicsGene expression changes during resistance toward vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitor (TKI) therapy in renal cell carcinoma (RCC)
This study was performed to understand the gene expression changes that accompany treatment of renal cell carcinoma (RCC) with vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitor (TKI) therapy. Human RCC cell lines were implanted into the flanks of nude beige mice, allowed...
ORGANISM(S): Homo sapiens 
2015-05-21 | E-GEOD-64052 | biostudies-arrayexpress
TranscriptomicsA receptor tyrosine kinase network comprised of FGFRs, EGFR, ERBB2, and MET drives growth and survival of HNSCC cell lines.
We have previously shown that some gefitinib insensitive head and neck squamous cell carcinoma (HNSCC) cell lines exhibit dominant autocrine fibroblast growth factor receptor (FGFR) signaling. Herein, we deployed a whole genome loss-of-function screen to identify genes whose knockdown potentiated th...
ORGANISM(S): Homo sapiens 
2013-05-03 | E-GEOD-39305 | biostudies-arrayexpress
GenomicsMartinostat as a Novel HDAC Inhibitor to Overcome Tyrosine Kinase Inhibitor Resistance in Chronic Myeloid Leukemia
Martinostat as a Novel HDAC Inhibitor to Overcome Tyrosine Kinase Inhibitor Resistance in Chronic Myeloid Leukemia
PRJNA1236844 | ENA
TranscriptomicsAn Inducible TGF-β2-TGFβR Pathway Modulates the Sensitivity of HNSCC Cells to Tyrosine Kinase Inhibitors Targeting Dominant Receptor Tyrosine Kinases
The epidermal growth factor receptor (EGFR) is overexpressed in approximately 90% of head and neck squamous cell carcinomas (HNSCC), and molecularly targeted therapy against the EGFR with the monoclonal antibody cetuximab modestly increases overall survival in head and neck cancer patients. We hypot...
ORGANISM(S): Homo sapiens 
2016-03-22 | E-GEOD-67500 | biostudies-arrayexpress
ProteomicsTotal protein profiles of human induced pluripotent stem cell-derived cardiomyocytes in response to four tyrosine kinase inhibitors
Drug-induced cardiotoxicity is a widespread clinical issue affecting numerous drug classes and remains difficult to treat. One such drug class is Tyrosine Kinase Inhibitors (TKIs), which cause varying degrees of contraction-related cardiotoxicity usually after weeks of exposure. Understanding molecu...
ORGANISM(S): Homo sapiens (Human) 
2019-05-16 | PXD012043 | Pride
Tyrosine kinase inhibitor Cardiotoxicity Aerobic glycolysis Human induced pluripotent stem cell-derived cardiomyocyte Mitochondrial respiration Drug adaptation Tandem mass tag mass spectrometry 
GenomicsMultiscale profiling of tyrosine kinase inhibitor cardiotoxicity reveals mechanosensitive ion channel PIEZO1 as cardioprotective
Multiscale profiling of tyrosine kinase inhibitor cardiotoxicity reveals mechanosensitive ion channel PIEZO1 as cardioprotective
PRJNA1209102 | ENA
ProteomicsProbing tyrosine kinase inhibitors specificity
Using a three-pronged MS-based proteomic approach, we assessed the mode-of-action of four clinically-relevant tyrosine kinase inhibitors in an epithelial cancer cell line. Here we defined the: (I) semi-quantitative tyrosine kinome; (II) drug interactome; and (III) drug-induced effects on the tyrosin...
ORGANISM(S): Homo sapiens (Human) 
2014-05-12 | PXD000681 | Pride
Human Tyrosine kinase inhibitors Chemical proteomics Phosphoproteomics Phosphotyrosine Lc-ms/ms 
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