Sep 1, 2019 · Inhibition of EZH2 and HDAC is synergistic and leads to the dissociation of PRC2 complex. Our findings support the clinical translation of the combination of EZH2 and HDAC inhibition in EZH2 dysregulated lymphomas.

Dec 1, 2024 · Satisfyingly, compounds 22a and 22b were identified as potent HDACs/EZH2 dual inhibitors with robust antiproliferative activities against one diffuse large-cell B cell lymphomas (DLBCL) cell line harboring EZH2 mutation and multiple acute myeloid leukemia (AML) cell lines.

Nov 5, 2021 · Here, we utilize transcriptomic and flow cytometric methods to assess whether epigenetic remodeling with tazemetostat (EZH2 inhibitor) and belinostat (HDAC inhibitor) can alter the immunogenicity of GC-DLBCL.

Dec 2, 2016 · This data suggests that concomitant inhibition of EZH2 and HDAC is highly synergistic and leads to the dissociation of PRC2 complex. By releasing transcriptional inhibition key tumor suppressors and cell cycle regulators may be re-expressed.

Since the histone modifying enzymes EZH2 and HDACs control a number of epigenetic-dependent carcinogenic pathways, we designed the first-in-class dual EZH2/HDAC inhibitor 5 displaying (sub)micromolar inhibition against both targets.

Feb 27, 2024 · We show that hypoxia-activated XBP1s forms a stable repressor protein complex with HDAC2 and EZH2 to suppress ΔNp63α transcription. Notably, H3K27ac is predominantly occupied on the ΔNp63...

Sep 3, 2019 · Inhibition of EZH2 and HDAC is synergistic and leads to the dissociation of PRC2 complex. Our findings support the clinical translation of the combination of EZH2 and HDAC inhibition in EZH2 dysregulated lymphomas.

Aug 24, 2021 · The combination of HDAC inhibitor HBI8000 with EZH2 inhibitor SHR2554 exhibited dramatic anti-tumor activity in both mutant and wild-type DLBCL, which may become a potential therapeutic modality for the treatment of DLBCL patients.

Nov 23, 2021 · Here, we utilize transcriptomic and flow cytometric methods to assess whether epigenetic remodeling with tazemetostat (EZH2 inhibitor) and belinostat (HDAC inhibitor) can alter the immunogenicity of GC-DLBCL.

Aug 5, 2023 · EZH2 cooperates with HDAC in reprogramming histone acetylation and methylation, resulting in more permanent silencing of target genes. HDAC2 interacts with EZH2 to block EZH2/ARID1A target protein expression in ARID1A-mutant ovarian cancers.