Unknown,Transcriptomics,Genomics,Proteomics

Dataset Information

Comparison of gene expression alterations induced by distinct PI3K inhibitors

ABSTRACT: The goal is the characterization of the off-target activity of BKM120 observed in A2058 human melanoma cell line at IC90 concentration (3.606 ÂµM) but not at lower concentrations. Controls are BEZ235, GDC0941, showing no off-target activity. A secondary objective is the characterizations of drug effects on transcript expression with respect to a control treatment (DMSO) of those PI3K inhibitors. 3 compounds, 3 concentrations per compound treatment, DMSO control treatement, 4 biological replicates

ORGANISM(S): Homo sapiens

SUBMITTER: Saskia Brachmann

PROVIDER: E-GEOD-33643 | biostudies-arrayexpress |

REPOSITORIES: biostudies-arrayexpress

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Publications

Characterization of the mechanism of action of the pan class I PI3K inhibitor NVP-BKM120 across a broad range of concentrations.

Brachmann Saskia M SM Kleylein-Sohn Julia J Gaulis Swann S Kauffmann Audrey A Blommers Marcel J J MJ Kazic-Legueux Malika M Laborde Laurent L Hattenberger Marc M Stauffer Fabian F Vaxelaire Juliane J Romanet Vincent V Henry Chrystèle C Murakami Masato M Guthy Daniel Alexander DA Sterker Dario D Bergling Sebastian S Wilson Christopher C Brümmendorf Thomas T Fritsch Christine C Garcia-Echeverria Carlos C Sellers William R WR Hofmann Francesco F Maira Sauveur-Michel SM

Molecular cancer therapeutics 20120531 8

The pan-phosphoinositide 3-kinase (PI3K) inhibitor BKM120 was found, at high concentrations, to cause cell death in various cellular systems, irrespective of their level of PI3K addiction. Transcriptional and biochemical profiling studies were used to identify the origin of these unexpected and apparently PI3K-independent effects. At 5- to 10-fold, the concentration needed to half-maximally inhibit PI3K signaling. BKM120 treatment caused changes in expression of mitotic genes and the induction o ...[more]

PMID: 22653967

Dataset Information

Comparison of gene expression alterations induced by distinct PI3K inhibitors

Publications

Characterization of the mechanism of action of the pan class I PI3K inhibitor NVP-BKM120 across a broad range of concentrations.

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