Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells

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The long non-coding RNAHOTAIRis transcriptionally activated by HOXA9 and is an independent prognostic marker in patients with malignant glioma

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Targeting Histone Modifications in Breast Cancer: A Precise Weapon on the Way

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Attenuation of SARS‐CoV‐2 replication and associated inflammation by concomitant targeting of viral and host cap 2'‐O‐ribose methyltransferases

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Preclinical pharmacokinetic studies of 3-deazaneplanocin A, a potent epigenetic anticancer agent, and its human pharmacokinetic prediction using GastroPlus™

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Overexpression of MYC and EZH2 cooperates to epigenetically silence MST1 expression

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Epigenetic Mechanisms in Commonly Occurring Cancers

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Novel insights into chromosomal conformations in cancer

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Aberrant methylation and decreased expression of the TGF‐β/Smad target gene FBXO32 in esophageal squamous cell carcinoma

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Knockdown of RNF2 induces cell cycle arrest and apoptosis in prostate cancer cells through the upregulation of TXNIP

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Epigenetic Activation of Pro-angiogenic Signaling Pathways in Human Endothelial Progenitors Increases Vasculogenesis

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EZH2 regulates dental pulp inflammation by direct effect on inflammatory factors

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DNMT1 modulates interneuron morphology by regulatingPak6expression through crosstalk with histone modifications

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The tumor suppressor microRNA-101 becomes an epigenetic player by targeting the Polycomb group protein EZH2 in cancer

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Inhibition of histone methyltransferase EZH 2 depletes leukemia stem cell of mixed lineage leukemia fusion leukemia through upregulation of p16

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The protein tyrosine phosphatase receptor type R gene is an early and frequent target of silencing in human colorectal tumorigenesis

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EZH2-Induced H3K27me3 is Associated with Epigenetic Repression of the ARHI Tumor-Suppressor Gene in Ovarian Cancer

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Antitumor effects of pharmacological EZH2 inhibition on malignant peripheral nerve sheath tumor through the miR-30a and KPNB1 pathway

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Pituitary tumours: all silent on the epigenetics front

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Molecular Pathways: Epigenetic Modulation of Wnt–Glycogen Synthase Kinase-3 Signaling to Target Human Cancer Stem Cells

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Implications of Epigenetic Mechanisms and their Targets in Cerebral Ischemia Models

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Loss of enhancer of zeste homologue 2 (EZH2) at tumor invasion front is correlated with higher aggressiveness in colorectal cancer cells

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Histone modification and histone modification-targeted anti-cancer drugs in breast cancer: Fundamentals and beyond

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Long-term Stability of Demethylation after Transient Exposure to 5-Aza-2′-Deoxycytidine Correlates with Sustained RNA Polymerase II Occupancy

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Targeting Enhancer of Zeste Homolog 2 as a promising strategy for cancer treatment

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Enhancer of Zeste Homolog 2 Is a Negative Regulator of Mitochondria-Mediated Innate Immune Responses

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FMR1 Reactivating Treatments in Fragile X iPSC-Derived Neural Progenitors In Vitro and In Vivo

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Comparison of gene expression profiles reveals aberrant expression of FOXO1, Aurora A/B and EZH2 in lesional psoriatic skins

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Role of the histone H 3 lysine 9 methyltransferase S uv39 h1 in maintaining E psteinn– B arr virus latency in B 95–8 cells

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Epigenetic modification of the Epstein-Barr virus BZLF1 promoter regulates viral reactivation from latency

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An evolutionarily conserved PTEN-C/EBPα-CTNNA1 axis controls myeloid development and transformation

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Enhancer of zeste homolog 2 (EZH2) in pediatric soft tissue sarcomas: first implications

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Genetic and Epigenetic Modulation of Drug Resistance in Cancer: Challenges and Opportunities

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EZH2 is required for mouse oocyte meiotic maturation by interacting with and stabilizing spindle assembly checkpoint protein BubRI

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EZH2: The roles in targeted therapy and mechanisms of resistance in breast cancer

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Elevated expression of long intergenic non‐coding RNA HOTAIR in a basal‐like variant of MCF‐7 breast cancer cells

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Determinants of Sensitivity to DZNep Induced Apoptosis in Multiple Myeloma Cells

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Methylation modification in gastric cancer and approaches to targeted epigenetic therapy (Review)

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Aberrant Epigenetic Regulation in Head and Neck Cancer Due to Distinct EZH2 Overexpression and DNA Hypermethylation

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Understanding and Targeting Apoptotic Pathways in Ovarian Cancer

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Long non-coding RNAs in recurrent ovarian cancer: Theranostic perspectives

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EZH2 Inhibition Interferes With the Activation of Type I Interferon Signaling Pathway and Ameliorates Lupus Nephritis in NZB/NZW F1 Mice

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Marginal zone lymphoma: old, new, targeted, and epigenetic therapies

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Epigenetic Cancer Prevention Mechanisms in Skin Cancer

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Mutation Spectra of Histone Methyltransferases With Canonical SET Domains and EZH2-Targeted Therapy

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Polycomb Group Protein Ezh2 Regulates Hepatic Progenitor Cell Proliferation and Differentiation in Murine Embryonic Liver

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Genistein Enhances Radiosensitivity of Human Hepatocellular Carcinoma Cells by Inducing G2/M Arrest and Apoptosis

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Epigenetic mechanisms of protein tyrosine phosphatase 6 suppression in diffuse large B-cell lymphoma: implications for epigenetic therapy

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Epigenetic Control of Ccr7 Expression in Distinct Lineages of Lung Dendritic Cells

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Epigenetic reprogramming in breast cancer: From new targets to new therapies

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Gene set-based module discovery in the breast cancer transcriptome

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Differential expression of enhancer of zeste homolog 2 (EZH2) protein in small cell and aggressive B-cell non-Hodgkin lymphomas and differential regulation of EZH2 expression by p-ERK1/2 and MYC in aggressive B-cell lymphomas

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The cancer-associated CTCFL/BORIS protein targets multiple classes of genomic repeats, with a distinct binding and functional preference for humanoid-specific SVA transposable elements

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Inhibition of EZH2 primes the cardiac gene activation via removal of epigenetic repression during human direct cardiac reprogramming

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Epigenetic alterations of the keratin 13 gene in oral squamous cell carcinoma

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Roles of enhancer of zeste homolog 2: From skeletal muscle differentiation to rhabdomyosarcoma carcinogenesis

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Quantitative Histone Mass Spectrometry Identifies Elevated Histone H3 Lysine 27 (Lys27) Trimethylation in Melanoma

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Over expression of miR-200c suppresses invasion and restores methotrexate sensitivity in lung cancer A549 cells

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Nicotine associated breast cancer in smokers is mediated through high level of EZH2 expression which can be reversed by methyltransferase inhibitor DZNepA

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Epigenetic modulation by small molecule compounds for neurodegenerative disorders

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S-adenosylhomocysteine (AdoHcy)-dependent methyltransferase inhibitor DZNep overcomes breast cancer tamoxifen resistance via induction of NSD2 degradation and suppression of NSD2-driven redox homeostasis

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Epigenetic Targeting Therapies to Overcome Chemotherapy Resistance

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16-Hydroxycleroda-3,13-dien-15,16-olide regulates the expression of histone-modifying enzymes PRC2 complex and induces apoptosis in CML K562 cells

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Small molecule epigenetic inhibitors targeted to histone lysine methyltransferases and demethylases

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Mariner Transposons Contain a Silencer: Possible Role of the Polycomb Repressive Complex 2

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Epigenetic Modifications in Cutaneous Malignant Melanoma

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Emerging role of F-box proteins in the regulation of epithelial-mesenchymal transition and stem cells in human cancers

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Moonlighting Metabolic Enzymes in Cancer: New Perspectives on the Redox Code

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Linking epithelial-to-mesenchymal-transition and epigenetic modifications

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Transcriptional Repressive H3K9 and H3K27 Methylations Contribute to DNMT1-Mediated DNA Methylation Recovery

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Molecular Pathways: The Complexity of the Epigenome in Cancer and Recent Clinical Advances

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Can a Metastatic Gene Expression Profile Outperform Tumor Size as a Predictor of Occult Lymph Node Metastasis in Oral Cancer Patients?

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Pharmacologic down-regulation of EZH2 suppresses bladder cancerin vitroandin vivo

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Human Papillomavirus Downregulates the Expression of IFITM1 and RIPK3 to Escape from IFNγ- and TNFα-Mediated Antiproliferative Effects and Necroptosis

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Emerging application of genomics-guided therapeutics in personalized lung cancer treatment

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Histone modifications and p53 binding poise the p21 promoter for activation in human embryonic stem cells

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β-Arrestin1 promotes the progression of chronic myeloid leukaemia by regulating BCR/ABL H4 acetylation

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Recent Advances about the Applications of Click Reaction in Chemical Proteomics

Yao, T., Xu, X., & Huang, R. (2021) · Molecules · doi:10.3390/molecules26175368 · Cited by 28

Jmjd3 activates Mash1 gene in RA‐induced neuronal differentiation of P19 cells

Dai, J., Lu, J., Zhang, Y., & Shen, Y. (2010) · Journal of Cellular Biochemistry · doi:10.1002/jcb.22703 · Cited by 29

Double sword role of EZH2 in leukemia

Safaei, S., Baradaran, B., Hagh, M. F., Alivand, M. R., Talebi, M., Gharibi, T., & Solali, S. (2017) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2017.12.059 · Cited by 29

Aberrant differential expression of EZH2 and H3K27me3 in extranodal NK/T-cell lymphoma, nasal type, is associated with disease progression and prognosis

Liu, J., Li, L., Huang, S., Nong, L., Li, D., Zhang, B., & Li, T. (2018) · Human Pathology · doi:10.1016/j.humpath.2018.08.025 · Cited by 29

De Novo Peptide Design and Experimental Validation of Histone Methyltransferase Inhibitors

Smadbeck, J. B., Peterson, M. B., Zee, B. M., Garapaty, S., Mago, A., Lee, C., Giannis, A., Trojer, P., Garcia, B. A., & Floudas, C. A. (2014) · PLoS ONE · doi:10.1371/journal.pone.0090095 · Cited by 28

The role of epigenetic regulation in stem cell and cancer biology

van Vlerken, L. E., Hurt, E. M., & Hollingsworth, R. E. (2012) · Journal of Molecular Medicine · doi:10.1007/s00109-012-0917-9 · Cited by 29

Epigenetic control of CCR5 transcript levels in immune cells and modulation by small molecules inhibitors

Wierda, R. J., Kuipers, H. F., van Eggermond, M. C. J. A., Benard, A., van Leeuwen, J. C., Carluccio, S., Geutskens, S. B., Jukema, J. W., Márquez, V. E., Quax, P. H. A., et al. (2011) · Journal of Cellular and Molecular Medicine · doi:10.1111/j.1582-4934.2011.01482.x · Cited by 28

DZNep inhibits the proliferation of colon cancer HCT116 cells by inducing senescence and apoptosis

Sha, M.-Q., Mao, G., Wang, G., Chen, Y., Wu, X., & Wang, Z. (2015) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2015.01.011 · Cited by 28

Functional and therapeutic significance of EZH2 in urological cancers

Liu, X., Wu, Q., & Li, L. (2017) · Oncotarget · doi:10.18632/oncotarget.16765 · Cited by 28

Antihistamine Drug Ebastine Inhibits Cancer Growth by Targeting Polycomb Group Protein EZH2

Li, Q., Liu, K. Y., Liu, Q., Wang, G., Jiang, W., Meng, Q., Yang, Y., Yang, Y., Wang, R., Zhu, S. L., et al. (2020) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-20-0250 · Cited by 28

PRIMA-1, a Mutant p53 Reactivator, Restores the Sensitivity of TP53 Mutant-Type Thyroid Cancer Cells to the Histone Methylation Inhibitor 3-Deazaneplanocin A

Cui, B., Yang, Q., Guan, H., Shi, B., Hou, P., & Ji, M. (2014) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jc.2013-3147 · Cited by 28

EZH2 is increased in paediatric T-cell acute lymphoblastic leukemia and is a suitable molecular target in combination treatment approaches

D’Angelo, V., Iannotta, A., Ramaglia, M., Lombardi, A., Zarone, M. R., Desiderio, V., Affinita, M. C., Pecoraro, G., Martino, M. D., Indolfi, P., et al. (2015) · Journal of Experimental & Clinical Cancer Research · doi:10.1186/s13046-015-0191-0 · Cited by 28

Anti-leukemic effects of HDACi Belinostat and HMTi 3-Deazaneplanocin A on human acute promyelocytic leukemia cells

Valiulienė, G., Stirblytė, I., Jasnauskaitė, M., Borutinskaite, V. V., & Navakauskienė, R. (2017) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2017.02.014 · Cited by 28

F‑box proteins involved in cancer‑associated drug resistance (Review)

Gong, J., Zhou, Y., Liu, D., & Huo, J. (2018) · Oncology Letters · doi:10.3892/ol.2018.8500 · Cited by 28

Chromatin Modulation by Oncogenic Transcription Factors: New Complexity, New Therapeutic Targets

Hormaeche, I., & Licht, J. D. (2007) · Cancer Cell · doi:10.1016/j.ccr.2007.05.005 · Cited by 28

Analysis of the antiproliferative effects of 3-deazaneoplanocin A in combination with standard anticancer agents in rhabdoid tumor cell lines

Unland, R., Borchardt, C., Clemens, D., Kool, M., Dirksen, U., & Frühwald, M. C. (2014) · Anti-Cancer Drugs · doi:10.1097/cad.0000000000000181 · Cited by 27

Efficacy of EZH2 inhibitory drugs in human papillomavirus-positive and human papillomavirus-negative oropharyngeal squamous cell carcinomas

Lindsay, C., Kostiuk, M. A., Harris, J., O’Connell, D. A., Seikaly, H. R., & Biron, V. L. (2017) · Clinical Epigenetics · doi:10.1186/s13148-017-0390-y · Cited by 28

Downregulation of TrkB Expression and Signaling by Valproic Acid and Other Histone Deacetylase Inhibitors

Dedoni, S., Marras, L., Olianas, M. C., Ingianni, A., & Onali, P. (2019) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.119.258129 · Cited by 28

Methylation deficiency disrupts biological rhythms from bacteria to humans

Fustin, J., Ye, S., Rakers, C., Kaneko, K., Fukumoto, K., Yamano, M., Versteven, M., Grünewald, E., Cargill, S. J., Tamai, K. T., et al. (2020) · Communications Biology · doi:10.1038/s42003-020-0942-0 · Cited by 27

Pharmacological inhibition of polycomb repressive complex-2 activity induces apoptosis in human colon cancer stem cells

Benoit, Y. D., Witherspoon, M., Laursen, K. B., Guezguez, A., Beauséjour, M., Beaulieu, J., Lipkin, S. M., & Gudas, L. J. (2013) · Experimental Cell Research · doi:10.1016/j.yexcr.2013.04.006 · Cited by 50

DZNep may directly target putative cancer stem cells in biliary tract cancer cells by inhibition of PRC2

Mayr, C., Wagner, A. C., Stöcklinger, A., Jakab, M., Illig, R., Pichler, M., Berr, F., Neureiter, D., & Kiesslich, T. (2014) · Zeitschrift für Gastroenterologie · doi:10.1055/s-0034-1386189

Abstract 2016: Combined targeting of epigenetic mechanisms has superior efficacy against human mantle cell lymphoma cells

Fiskus, W. C., Sharma, S., Rao, R., Balusu, R., Tao, J., Sotomayor, E. M., Atadja, P. W., Ganguly, S., Bearss, D. J., & Bhalla, K. N. (2011) · Cancer Research · doi:10.1158/1538-7445.am2011-2016

Polycomb genes and cancer: Time for clinical application?

Crea, F., Paolicchi, E., Márquez, V. E., & Danesi, R. (2011) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2011.10.007 · Cited by 87

Abstract 5360: Targeting H3K27 Methylation by 3-Deazaneplanocin A (DZNep) in lung and esophageal cancers.

Rao, M., Hong, Y., Atay, S. M., Upham, T. C., Hong, J. A., Datrice, N., Zhang, M. F., Zudaire, E., Márquez, V. E., & Schrump, D. S. (2013) · Cancer Research · doi:10.1158/1538-7445.am2013-5360 · Cited by 3