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    GENE:

    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit)

    i
    Other names: EZH2, ENX-1, EZH1, KMT6, KMT6A, Enhancer of zeste 2 polycomb repressive complex 2 subunit
    2d
    Molecular Effect of Tobacco on Genetic, Epigenetic, and Metabolic Pathways During Cancer Progression. (PubMed, Cureus)
    These findings underscore the need for targeted interventions, such as epigenetic therapies, metabolic reprogramming, and robust tobacco control policies, to mitigate the global burden of tobacco-related diseases. By providing a unified framework for understanding tobacco's molecular impact, this research advocates for precision medicine and public health strategies to address the pervasive effects of tobacco on human health.
    Review • Journal • PARP Biomarker • IO biomarker
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    BCL2 (B-cell CLL/lymphoma 2) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • TERT (Telomerase Reverse Transcriptase) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • HIF1A (Hypoxia inducible factor 1, alpha subunit) • ATR (Ataxia telangiectasia and Rad3-related protein) • PARP1 (Poly(ADP-Ribose) Polymerase 1) • MTHFR (Methylenetetrahydrofolate Reductase) • SOX2 • CASP3 (Caspase 3) • POU5F1 (POU Class 5 Homeobox 1) • CASP9 (Caspase 9) • HDAC1 (Histone Deacetylase 1) • YBX1 (Y-Box Binding Protein 1) • NANOG (Nanog Homeobox) • DRD2 (Dopamine Receptor D2) • SUV39H1 (SUV39H1 Histone Lysine Methyltransferase) • TCF4 (Transcription Factor 4) • COMT (Catechol-O-Methyltransferase)
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    TP53 mutation
    4d
    EZH2 inhibition overcomes immune evasion in lung adenocarcinoma by restoring CCL5-mediated T-cell recruitment and MHC class I antigen presentation. (PubMed, Acta Biochim Biophys Sin (Shanghai))
    In conclusion, EZH2 overexpression promotes immune evasion in LUAD by suppressing CCL5-mediated T-cell recruitment and MHC class I antigen presentation. Targeting EZH2 augments antitumor immunity, supporting its therapeutic potential in combination immunotherapy strategies.
    Journal • PD(L)-1 Biomarker • IO biomarker
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    PD-L1 (Programmed death ligand 1) • CD8 (cluster of differentiation 8) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • CCL5 (Chemokine (C-C motif) ligand 5)
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    PD-L1 overexpression
    7d
    EZH2 Expression Is Associated With Sensitivity to Inhibitors and Promotes Malignancy in Endometrial Cancer Cells. (PubMed, Anticancer Res)
    EZH2 plays a crucial role in promoting malignant phenotypes in EC, and its expression level correlates with cellular sensitivity to EZH2 inhibitors. These findings suggest that EZH2 could serve as a valuable therapeutic target and predictive biomarker for personalized medicine in EC.
    Journal
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit)
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    Tazverik (tazemetostat) • GSK2816126 • EPZ005687 • lirametostat (CPI-1205)
    9d
    [Retracted] MicroRNA-298 inhibits malignant phenotypes of epithelial ovarian cancer by regulating the expression of EZH2. (PubMed, Oncol Lett)
    [This retracts the article DOI: 10.3892/ol.2016.5204.].
    Journal
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit)
    10d
    Therapeutic Horizons in Targeting EZH2 With Dual and Non-PROTAC Inhibitor Molecules: Recent Achievements, Comparative Analysis, and Future Perspectives. (PubMed, Arch Pharm (Weinheim))
    Conversely, multitarget hybrids such as Olaparib-Tazemetostat (33) and Tazemetostat-resorcinol (170) maintained robust cellular efficacy through synergistic epigenetic and DNA-repair modulation. Future perspectives emphasize rational design strategies integrating dual targeting, computational modeling, and covalent functionalities to enhance therapeutic durability. Collectively, these advances explain the evolving therapeutic horizon of non-PROTAC and dual EZH2 inhibitors, offering an outline for next-generation EZH2 inhibitors.
    Clinical • Review • Journal • PARP Biomarker
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • PARP1 (Poly(ADP-Ribose) Polymerase 1) • BRD4 (Bromodomain Containing 4) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
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    Lynparza (olaparib) • Tazverik (tazemetostat)
    11d
    Porphyromonas gingivalis promotes oral squamous cell carcinoma progression via the IL-6/EZH2/Snai2 axis. (PubMed, Sci Rep)
    Our study revealed a novel IL-6/EZH2/Snai2 signaling axis, which connected the P.g. infection, IL-6 upregulation, abnormal expression of EZH2 and Snai2, and OSCC progression. This study filled the gap of molecular mechanisms underlying P.g.-induced OSCC invasion and metastasis, providing a potential therapeutic target for inhibiting OSCC progression.
    Journal
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • IL6 (Interleukin 6) • SNAI2 (Snail Family Transcriptional Repressor 2)
    15d
    Epigenetic regulation of NDGA and its synergistic inhibition with EZH2 inhibitors in prostate cancer via NRP1. (PubMed, Acta Pharmacol Sin)
    On the other hand, NDGA inhibited CBP/p300, decreased H3K27ac levels, and synergized with the EZH2 inhibitor EPZ6438 against PC3 cells. In conclusion, NDGA is a potential epigenetic antineoplastic agent that downregulates EZH2 and H3K27me3 through the NRP1 and PI3K/AKT/mTOR pathways and exerts a synergistic antitumor effect with H3K27ac and EZH2 inhibitors, suggesting that it could be a valuable therapeutic option for prostate cancer.
    Journal
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • NRP1 (Neuropilin 1) • E2F1 (E2F transcription factor 1)
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    Tazverik (tazemetostat)
    16d
    Integrative bulk and single-cell transcriptomics link EZH2 to immunosuppressive programs and tumor-Treg crosstalk in castration-resistant prostate cancer. (PubMed, Front Immunol)
    For perturbation, the EZH2 inhibitor tazemetostat was evaluated in the CRPC-relevant C42 cell line with H3K27me3 readouts and transcriptomic profiling, with key changes validated by RT-qPCR...This multi-layer integrative analysis suggests that EZH2 is associated with proliferative malignant states and immunosuppressive microenvironment features in advanced PCa, including Treg-linked crosstalk. Transcriptomic profiling following EZH2 inhibition supports modulation of these programs by EZH2-targeted perturbation, while functional and causal mechanisms warrant further investigation.
    Journal
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • PLCG2 (Phospholipase C Gamma 2) • SOCS3 (Suppressor Of Cytokine Signaling 3) • TIMP3 (TIMP Metallopeptidase Inhibitor 3)
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    Tazverik (tazemetostat)
    16d
    Ancestrally diverse autologous patient-derived organoid - immune cell co-culture platform for addressing immunotherapeutic outcome disparities in high-grade endometrial cancer. (PubMed, Cancer Res Commun)
    Finally, this platform enabled evaluation of the safety and efficacy of emerging immunotherapies, including protease-activatable bispecific T-cell engagers (TCEs) and EGFR-targeted chimeric antigen receptor (CAR) T cells. Together, this sustainable, scalable, ancestrally diverse autologous PDO-immune cell co-culture platform offers a robust resource for dissecting immune evasion mechanisms and accelerating the development of new immunotherapies to address disparities in endometrial cancer outcomes.
    Journal • IO biomarker
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • IFNG (Interferon, gamma)
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    MSI-H/dMMR
    17d
    2024/3993 EZHiSWITCH: An open label phase II platform modular study exploring the efficacy and safety of the Valemetostat (EZH1/2 inhibitor) in patients with selected solid tumors. (2024-519788-16-00)
    P1/2, N=600, Not yet recruiting, Institut Gustave Roussy
    New P1/2 trial
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    ARID1A (AT-rich interaction domain 1A) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • PBRM1 (Polybromo 1) • BAP1 (BRCA1 Associated Protein 1) • SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1) • SMARCA2 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily A, Member 2)
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    Ezharmia (valemetostat)
    22d
    Paediatric Therapeutic Development Workshop on rhabdoid tumours. (PubMed, Br J Cancer)
    Mouse double minute 2 homologue (MDM2) is a priority target for novel therapeutic development and combination trials. Combinations of EZH2, MDM2 inhibitors and selective inhibitors of nuclear export should be evaluated robustly preclinically and drive early clinical studies.
    Review • Journal
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    FGFR (Fibroblast Growth Factor Receptor) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • SMARCA4 (SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily A, member 4) • SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1) • DDB1 (Damage Specific DNA Binding Protein 1)
    23d
    Dual Effect of EZH2 Gene Editing with CRISPR/Cas9 in Lung Cancer. (PubMed, Biology (Basel))
    In this study, EZH2 levels were modulated by CRISPR/Cas9 gene editing and PRC2 activity was inhibited with EZH2 inhibitor EPZ6438 or EED inhibitor MAK683. This was accompanied by increased expression of other PcG genes, including EZH1, CBX2, RING1, EED, and SUZ12, suggesting a compensatory interaction between PRC2 and PRC1 complexes. These findings provide significant clinical relevance, both in elucidating the mechanisms of novel molecular targets and in guiding treatment strategies for lung cancer when using epigenetic inhibitors.
    Journal
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • FOXA2 (Forkhead Box A2) • CBX2 (Chromobox 2) • SUZ12 (SUZ12 Polycomb Repressive Complex 2 Subunit)
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    Tazverik (tazemetostat) • MAK683