Quantification of Histone H3 Lys27 Trimethylation (H3K27me3) by High-Throughput Microscopy Enables Cellular Large-Scale Screening for Small-Molecule EZH2 Inhibitors

EZH2 inhibition can decrease global histone H3 lysine 27 trimethylation (H3K27me3) and thereby reactivates silenced tumor suppressor genes. Inhibition of EZH2 is regarded as an option for therapeutic cancer intervention. To identify novel small-molecule (SMOL) inhibitors of EZH2 in drug discovery, t...

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Veröffentlicht in:	Journal of biomolecular screening 2015-02, Vol.20 (2), p.190-201
Hauptverfasser:	Luense, Svenja, Denner, Philip, Fernández-Montalván, Amaury, Hartung, Ingo, Husemann, Manfred, Stresemann, Carlo, Prechtl, Stefan
Format:	Artikel
Sprache:	eng
Schlagworte:	Automation, Laboratory Cell Cycle - drug effects Cell Line, Tumor Dose-Response Relationship, Drug Drug Discovery Enhancer of Zeste Homolog 2 Protein Gene Knockdown Techniques High-Throughput Screening Assays Histones - antagonists & inhibitors Histones - genetics Histones - metabolism Humans Inhibitory Concentration 50 Methylation - drug effects Microscopy Original Research Polycomb Repressive Complex 2 - antagonists & inhibitors RNA Interference Small Molecule Libraries Structure-Activity Relationship
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