Author: Véronique Della Valle

0000000000791640

AUTHOR

Véronique Della Valle

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Combined HAT/EZH2 modulation leads to cancer-selective cell death

2018

Contains fulltext : 197351.pdf (Publisher’s version ) (Open Access) Epigenetic alterations have been associated with both pathogenesis and progression of cancer. By screening of library compounds, we identified a novel hybrid epi-drug MC2884, a HAT/EZH2 inhibitor, able to induce bona fide cancer-selective cell death in both solid and hematological cancers in vitro, ex vivo and in vivo xenograft models. Anticancer action was due to an epigenome modulation by H3K27me3, H3K27ac, H3K9/14ac decrease, and to caspase-dependent apoptosis induction. MC2884 triggered mitochondrial pathway apoptosis by up-regulation of cleaved-BID, and strong down-regulation of BCL2. Even aggressive models of cancer, …

0301 basic medicineacetylation; apoptosis; cancer; epigenetics; methylation; oncologyProgrammed cell death[SDV.CAN]Life Sciences [q-bio]/Cancer03 medical and health sciencesacetylation; apoptosis; cancer; epigenetics; methylationIn vivomedicinecancerMolecular Biologyacetylationepigeneticsbusiness.industryCancer; Epigenetics; Apoptosis; Acetylation; MethylationEZH2apoptosisApoptosiEpigeneticCancerEpigenomemedicine.disease3. Good healthLeukemia030104 developmental biologyOncologyApoptosisCancer researchmethylationbusinessEx vivoResearch PaperOncotarget

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