Quantification of histone H3 lys27 trimethylation (H3K27me3) by high-throughput microscopy enables cellular large-scale screening for small-molecule EZH2 inhibitors

Journal of Biomolecular Screening

Volumn 20, Issue 2, 2015, Pages 190-201

  Luense, Svenja ^a   Denner, Philip ^a   Fernández Montalván, Amaury ^a   Hartung, Ingo ^a   Husemann, Manfred ^a   Stresemann, Carlo ^a   Prechtl, Stefan ^a  

^a BAYER PHARMA AG   (Germany)

Author keywords

chromatin modulators; EZH2; high content analysis; histone methyltransferase; KMT6

Indexed keywords

HISTONE H3; HISTONE H3 LYS27; PROTEIN INHIBITOR; SMALL INTERFERING RNA; SMALL MOLECULE TRANSCRIPTION FACTOR EZH2 INHIBITOR; TRANSCRIPTION FACTOR EZH2; UNCLASSIFIED DRUG; EZH2 PROTEIN, HUMAN; HISTONE; MOLECULAR LIBRARY; POLYCOMB REPRESSIVE COMPLEX 2;

ARTICLE; AUTOMATION; CELL DIFFERENTIATION; CELL LINE; CONTENT ANALYSIS; CONTROLLED STUDY; DNA METHYLATION; DRUG SCREENING; ELECTRONICS; EPIGENETICS; FEMALE; HELA CELL LINE; HIGH THROUGHPUT SCREENING; HISTONE METHYLATION; HISTONE TRIMETHYLATION; HUMAN; HUMAN CELL; LARGE SCALE PRODUCTION; LIMIT OF QUANTITATION; PHENOTYPE; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; ANTAGONISTS AND INHIBITORS; CELL CYCLE; DOSE RESPONSE; DRUG DEVELOPMENT; DRUG EFFECTS; GENE SILENCING; GENETICS; IC50; LABORATORY AUTOMATION; METABOLISM; METHYLATION; MICROSCOPY; MOLECULAR LIBRARY; RNA INTERFERENCE; TUMOR CELL LINE;

AUTOMATION, LABORATORY; CELL CYCLE; CELL LINE, TUMOR; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; GENE KNOCKDOWN TECHNIQUES; HIGH-THROUGHPUT SCREENING ASSAYS; HISTONES; HUMANS; INHIBITORY CONCENTRATION 50; METHYLATION; MICROSCOPY; POLYCOMB REPRESSIVE COMPLEX 2; RNA INTERFERENCE; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84921449922     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057114559668     Document Type: Article

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