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Analysis of whole genome expression change after NPD13668 treatment

ABSTRACT: EZH2 is a catalytic component of polycomb repressive complex 2 (PRC2), which contributes to aggressiveness in many types of cancers. Targeting EZH2/PRC2 has been challenged and now some inhibitors are under clinical trials for cancer treatments. Interestingly, anti-tumor effects of EZH2 is not always depend on H3K27 methyltransferase activity. In order to identify novel inhibitors against EZH2/PRC2, we established a chemical screening system based on measurement of reactivation of promoter activity, which is intrinsically silenced by EZH2/PRC2. We screened more than 300,000 small chemicals and identified 85 chemicals. After validation of reactivation of EZH2/PRC2 target genes, we identified chemical NPD13668 as a potential inhibitor of EZH2/PRC2 activity. To evaluate NPD13668 effect, we analysed whole genome expression change by using SurePrint G3 Human GE 8×60K array slides (G4851B, Agilent Technologies).

ORGANISM(S): Homo sapiens

PROVIDER: GSE122997 | GEO | 2019/02/01

REPOSITORIES: GEO

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