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• W2616420862 abstract "Abstract Cancer is associated with alterations in epigenetic mechanisms such as histone modifications and methylation of DNA, and inhibitors targeting epigenetic mechanisms represent a novel class of anti-cancer drugs. Neuroendocrine tumors (NETs) of the pancreas (PNETs) and bronchus (BNETs), which may have 5-year survivals of <50% and as low as 5%, respectively, represent targets for such drugs, as >40% of PNETs and ~35% of BNETs have mutations of the multiple endocrine neoplasia type 1 ( MEN1 ) gene, which encodes menin that modifies histones by interacting with histone methyltransferases. We assessed 9 inhibitors of epigenetic pathways, for their effects on proliferation, by CellTiter Blue assay, and apoptosis, by CaspaseGlo assay, using 1 PNET and 2 BNET cell lines. Two inhibitors, referred to as (+)-JQ1 (JQ1) and PFI-1, targeting the b romo and e xtra t erminal (BET) protein family which bind acetylated histone residues, were most effective in decreasing proliferation (by 40–85%, P <0.001) and increasing apoptosis (by 2–3.6 fold, P <0.001) in all 3 NET cell lines. The anti-proliferative effects of JQ1 and PFI-1 remained present for at least 48 hours after removal of the compound. JQ1, but not PFI-1, had cell cycle effects, assessed by propidium iodide staining and flow cytometry, resulting in increased and decreased proportions of NET cells in G1, and S and G2 phases, respectively. RNA Sequencing analysis revealed that these JQ1 effects were associated with increased histone 2B expression, and likely mediated through altered activity of bromodomain-containing (Brd) proteins. Assessment of JQ1 in vivo , using a pancreatic beta cell-specific conditional Men1 knockout mouse model that develops PNETs, revealed that JQ1 significantly reduced proliferation (by ~50%, P <0.0005), assessed by bromodeoxyuridine incorporation, and increased apoptosis (by ~3 fold, P <0.0005), assessed by terminal deoxynucleotidyl transferase dUTP nick end labelling, of PNETs. Thus, our studies demonstrate that BET protein inhibitors may provide new treatments for NETs." @default.
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• W2616420862 date "2017-05-15" @default.
• W2616420862 modified "2023-10-05" @default.
• W2616420862 title "Epigenetic pathway inhibitors represent potential drugs for treating pancreatic and bronchial neuroendocrine tumors" @default.
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• W2616420862 doi "https://doi.org/10.1038/oncsis.2017.30" @default.
• W2616420862 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5523063" @default.
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