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Targeting EZH2 in SMARCB1-deficient sarcomas: Advances and opportunities to potentiate the efficacy of EZH2 inhibitors

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Role of EZH2 in Epithelial Ovarian Cancer: From Biological Insights to Therapeutic Target

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Inhibition of DNA and Histone Methylation by 5-Aza-2′-Deoxycytidine (Decitabine) and 3-Deazaneplanocin-A on Antineoplastic Action and Gene Expression in Myeloid Leukemic Cells

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EZH2 promotes neoplastic transformation through VAV interaction-dependent extranuclear mechanisms

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Structures of histone methyltransferase SET7/9 in complexes with adenosylmethionine derivatives

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Sorafenib suppresses growth and survival of hepatoma cells by accelerating degradation of enhancer of zeste homolog 2

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Nuclear Morphometry, Epigenetic Changes, and Clinical Relevance in Prostate Cancer

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Acquired platinum resistance involves epithelial to mesenchymal transition through ubiquitin ligase FBXO32 dysregulation

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Aging and Age-Related Epigenetic Drift in the Pathogenesis of Leukemia and Lymphomas: New Therapeutic Targets

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The specific alteration of histone methylation profiles by DZNep during early zebrafish development

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Quantification of Histone H3 Lys27 Trimethylation (H3K27me3) by High-Throughput Microscopy Enables Cellular Large-Scale Screening for Small-Molecule EZH2 Inhibitors

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Aristeromycin and DZNeP cause growth inhibition of prostate cancer via induction of mir-26a

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Overcoming EZH2 Inhibitor Resistance by Taxane in PTEN-Mutated Cancer

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Inhibition of Polycomb Repressive Complex 2 activity reduces trimethylation of H3K27 and affects development in Arabidopsis seedlings

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Small Molecules Targeting H3K9 Methylation Prevent Silencing of Reactivated FMR1 Alleles in Fragile X Syndrome Patient Derived Cells

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Epigenetic aspects of MDS and its molecular targeted therapy

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Enhancer of zeste homolog 2 is overexpressed and contributes to epigenetic inactivation of p21 and phosphatase and tensin homolog in B-cell acute lymphoblastic leukemia

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Epigenetic therapy of hematological malignancies: where are we now?

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BCR/ABL increases EZH2 levels which regulates XIAP expression via miRNA-219 in chronic myeloid leukemia cells

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The role of enhancer of zeste homolog 2: From viral epigenetics to the carcinogenesis of hepatocellular carcinoma

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GSK343 induces autophagy and downregulates the AKT/mTOR signaling pathway in pancreatic cancer cells

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Epigenetic Changes in Cancer as Potential Targets for Prophylaxis and Maintenance Therapy

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Epigenetic dysregulation in hepatocellular carcinoma: focus on polycomb group proteins

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EZH2 as a Potential Target for NAFLD Therapy

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Cell-penetrating H4 tail peptides potentiate p53-mediated transactivation via inhibition of G9a and HDAC1

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Promoter methylation patterns in R ichter syndrome affect stem‐cell maintenance and cell cycle regulation and differ from de novo diffuse large B ‐cell lymphoma

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EZH2, an on–off valve in signal network of tumor cells

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Deregulation of polycomb repressor complex 1 modifier AUTS2 in T-cell leukemia

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Inhibition of EZH2 expression is associated with the proliferation, apoptosis, and migration of SW620 colorectal cancer cells in vitro

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p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma.

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Polycomb group proteins in cancer: multifaceted functions and strategies for modulation

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Epigenetic suppression of PGC1α (PPARGC1A) causes collateral sensitivity to HMGCR-inhibitors within BRAF-treatment resistant melanomas

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EZH2 ‐associated tumor malignancy: A prominent target for cancer treatment

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PRC2 regulates RNA polymerase III transcribed non-translated RNA gene transcription through EZH2 and SUZ12 interaction with TFIIIC complex

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The knock-down of overexpressed EZH2 and BMI-1 does not prevent osteosarcoma growth

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FBXO32, a new TGF-β/Smad signaling pathway target gene, is epigenetically inactivated in gastric cardia adenocarcinoma

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Pyrazole-based inhibitors of enhancer of zeste homologue 2 induce apoptosis and autophagy in cancer cells

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Chromatin remodeling by the histone methyltransferase EZH2 drives lung pre-malignancy and is a target for cancer prevention

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MicroRNA regulation of F-box proteins and its role in cancer

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Epigenetic regulation of retinal development and disease

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Polycomb and the Emerging Epigenetics of Pancreatic Cancer

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dDsk2 regulates H2Bub1 and RNA polymerase II pausing at dHP1c complex target genes

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The role of histone methyltransferase EZH2 in myelodysplastic syndromes

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The sunset of somatic genetics and the dawn of epigenetics: a new frontier in pancreatic cancer research

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BCL11A Promotes the Progression of Laryngeal Squamous Cell Carcinoma

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Identification of Polycomb Group Protein EZH2-Mediated DNA Mismatch Repair Gene MSH2 in Human Uterine Fibroids

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Sequential changes in histone modifications shape transcriptional responses underlying microglia polarization by glioma

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The Clinicopathological Significance of Epithelial Mesenchymal Transition Associated Protein Expression in Head and Neck Squamous Cell Carcinoma

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Epigenetic dysregulation of key developmental genes in radiation‐induced rat mammary carcinomas

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Genome-wide expression analysis reveals six contravened targets of EZH2 associated with breast cancer patient survival

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Wedelolactone inhibits human cytomegalovirus replication by targeting distinct steps of the viral replication cycle

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Combating the Epigenome: Epigenetic Drugs Against Non-Hodgkin‘S Lymphoma

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PRC2: an epigenetic multiprotein complex with a key role in the development of rhabdomyosarcoma carcinogenesis

Zoroddu, S., Marchesi, I., & Bagella, L. (2021) · Clinical Epigenetics · doi:10.1186/s13148-021-01147-w · Cited by 20

Histone 3 Lysine 27 Trimethylation Signature in Breast Cancer

Borkiewicz, L. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms222312853 · Cited by 20

Focus on the classical and non-classical functions of EZH2: Guide the development of inhibitors and degraders

Zhang, Q., Yang, H., Feng, Q., Cao, J., Zhang, Y., Li, L., & Yu, L. (2022) · Pharmacological Research · doi:10.1016/j.phrs.2022.106159 · Cited by 20

Synthesis of Neplanocin A and Its 3′-Epimer via an Intramolecular Baylis–Hillman Reaction

Tan, Y. X., Santhanakrishnan, S., Yang, H., Chai, C. L. L., & Tam, E. K. W. (2014) · The Journal of Organic Chemistry · doi:10.1021/jo501248e · Cited by 20

Co-expression of Bmi1 and EZH2 as an independent poor prognostic factor in esophageal squamous cell carcinoma

Ha, S. Y., & Kim, S. (2012) · Pathology - Research and Practice · doi:10.1016/j.prp.2012.05.012 · Cited by 20

Computational genomic analysis of PARK7 interactome reveals high BBS1 gene expression as a prognostic factor favoring survival in malignant pleural mesothelioma

Vavougios, G. D., Solenov, E. I., Hatzoglou, C., Baturina, G. S., Каткова, Л. Е., Molyvdas, P. A., Gourgoulianis, K. I., & Zarogiannis, S. G. (2015) · American Journal of Physiology-Lung Cellular and Molecular Physiology · doi:10.1152/ajplung.00051.2015 · Cited by 19

In silico and experimental analyses predict the therapeutic value of an EZH2 inhibitor GSK343 against hepatocellular carcinoma through the induction of metallothionein genes

Liu, T., Hong, Y.-H., Tung, K., & Yang, P. (2016) · Oncoscience · doi:10.18632/oncoscience.285 · Cited by 20

A functional single nucleotide polymorphism of SET8 is prognostic for breast cancer

Liu, B., Zhang, X., Song, F., Liu, Q., Dai, H., Zheng, H., Cui, P., Zhang, L., Zhang, W., & Chen, K. (2016) · Oncotarget · doi:10.18632/oncotarget.9099 · Cited by 20

Novel therapeutic strategies for MLL-rearranged leukemias

Wong, N.-H. M., & So, C. W. E. (2020) · Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms · doi:10.1016/j.bbagrm.2020.194584 · Cited by 20

Epigenetic Control of Osteoblast Differentiation by Enhancer of Zeste Homolog 2 (EZH2)

Dudakovic, A., & van Wijnen, A. J. (2017) · Current Molecular Biology Reports · doi:10.1007/s40610-017-0064-8 · Cited by 20

EZH2-inhibitor DZNep enhances apoptosis of renal tubular epithelial cells in presence and absence of cisplatin

Chen, S., Li, J., Wang, X., Lei, W., Li, H., Wan, J., Hu, Z., Zou, Y.-W., Wu, X., & Niu, H. (2020) · Cell Division · doi:10.1186/s13008-020-00064-3 · Cited by 20

Polycomb and Trithorax Group Proteins: The Long Road from Mutations in Drosophila to Use in Medicine

Chetverina, D., Ломаев, Д. В., & Erokhin, M. (2020) · Acta Naturae · doi:10.32607/actanaturae.11090 · Cited by 18

Critical Roles of Polycomb Repressive Complexes in Transcription and Cancer

Dong, G., Xu, J., Qi, Y.-R., Yuan, Z., & Zhao, W. H. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms23179574 · Cited by 21

Targeting epigenetic regulation for cancer therapy using small molecule inhibitors

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Chromatin access regulates the formation of Müller glia‐derived progenitor cells in the retina

Campbell, W. A., El‐Hodiri, H. M., Torres, D., Hawthorn, E. C., Kelly, L. E., Volkov, L. I., Akanonu, D., & Fischer, A. J. (2023) · Glia · doi:10.1002/glia.24366 · Cited by 19

Pre-Clinical Studies of Epigenetic Therapies Targeting Histone Modifiers in Lung Cancer

Huffman, K. E., & Martínez, E. D. (2013) · Frontiers in Oncology · doi:10.3389/fonc.2013.00235 · Cited by 19

Functional Characterization of D9, a Novel Deazaneplanocin A (DZNep) Analog, in Targeting Acute Myeloid Leukemia (AML)

Jiang, X., Lim, C. Z. H., Li, Z., Lee, P. L., Yatim, S. M. J. M., Guan, P., Li, J., Zhou, J., Pan, J., Chng, W. J., et al. (2015) · PLoS ONE · doi:10.1371/journal.pone.0122983 · Cited by 19

Differential Gene Expression Patterns Between Apical and Basal Inner Hair Cells Revealed by RNA-Seq

Tang, F. R., Chen, X., Jia, L., Li, H., Li, J., & Yuan, W. (2020) · Frontiers in Molecular Neuroscience · doi:10.3389/fnmol.2019.00332 · Cited by 19

Polycomb repressor complex 2 function in breast cancer (Review)

Martin, C., & Moorehead, R. A. (2020) · International Journal of Oncology · doi:10.3892/ijo.2020.5122 · Cited by 21

Epigenetic Regulation of Cell Signaling Pathways in Acute Lymphoblastic Leukemia

José‐Eneriz, E. S., Agirre, X., Rodríguez‐Otero, P., & Prósper, F. (2013) · Epigenomics · doi:10.2217/epi.13.56 · Cited by 19

Epigenetic mechanisms of plasticity and resistance in glioblastoma: therapeutic targets and implications

Amirmahani, F., Kumar, S., & Muthukrishnan, S. D. (2025) · Frontiers in Epigenetics and Epigenomics · doi:10.3389/freae.2025.1519449 · Cited by 18

Mitochondria-targeting nano therapy altering IDH2-mediated EZH2/EZH1 interaction as precise epigenetic regulation in glioblastoma

Kaundal, B., Karmakar, S., & Choudhury, S. R. (2022) · Biomaterials Science · doi:10.1039/d1bm02006d · Cited by 18

EZH2-mediated epigenetic silencing of tumor-suppressive let-7c/miR-99a cluster by hepatitis B virus X antigen enhances hepatocellular carcinoma progression and metastasis

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Apoptosis and DNA Methylation

Meng, H., Hackett, J. A., Nestor, C. E., Dunican, D. S., Madej, M. J., Reddington, J. P., Pennings, S., Harrison, D. J., & Meehan, R. R. (2011) · Cancers · doi:10.3390/cancers3021798 · Cited by 19

The role of polycomb repressive complexes in biliary tract cancer

Mayr, C., Neureiter, D., Wagner, A., Pichler, M., & Kiesslich, T. (2014) · Expert Opinion on Therapeutic Targets · doi:10.1517/14728222.2014.986460 · Cited by 18

Identification and Assessments of Novel and Potent Small-Molecule Inhibitors of EED–EZH2 Interaction of Polycomb Repressive Complex 2 by Computational Methods and Biological Evaluations

Zhu, K., Du, D., Yang, R. J., Tao, H., & Zhang, H. (2019) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.c19-00550 · Cited by 18

Epigenetic Silencing of Tumor Suppressor Genes in Pancreatic Cancer

Lomberk, G. A. (2011) · Journal of Gastrointestinal Cancer · doi:10.1007/s12029-011-9256-2 · Cited by 18

Integrative epigenome analysis identifies a Polycomb-targeted differentiation program as a tumor-suppressor event epigenetically inactivated in colorectal cancer

Tan, J. Y., Yang, X., Jiang, X., Zhou, J., Li, Z., Lee, P. L., Li, B., Robson, P., & Yu, Q. (2014) · Cell Death and Disease · doi:10.1038/cddis.2014.283 · Cited by 18

A NIR-responsive indocyanine green-genistein nanoformulation to control the polycomb epigenetic machinery for the efficient combinatorial photo/chemotherapy of glioblastoma

Kaundal, B., Srivastava, A. K., Sardoiwala, M. N., Karmakar, S., & Choudhury, S. R. (2019) · Nanoscale Advances · doi:10.1039/c9na00212j · Cited by 18

Loading 3-deazaneplanocin A into pegylated unilamellar liposomes by forming transient phenylboronic acid–drug complex and its pharmacokinetic features in Sprague–Dawley rats

Sun, F., Li, J., Yu, Q., & Chan, E. (2011) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2011.10.014 · Cited by 17

Disturbing the histone code in leukemia: translocations and mutations affecting histone methyl transferases

Chopra, M., & Bohlander, S. K. (2014) · Cancer Genetics · doi:10.1016/j.cancergen.2014.10.005 · Cited by 18

Development of second generation epigenetic agents

JONES, P. G. (2011) · MedChemComm · doi:10.1039/c1md00199j · Cited by 17

Rap1 and its regulatory proteins

Banerjee, R., Russo, N., Liu, M., Tubergen, E. V., & D’Silva, N. J. (2012) · Small GTPases · doi:10.4161/sgtp.20413 · Cited by 17

Identification of AHCY inhibitors using novel high-throughput mass spectrometry

Uchiyama, N., Dougan, D. R., Lawson, J. D., Kimura, H., Matsumoto, S.-I., Tanaka, Y., & Kawamoto, T. (2017) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2017.05.107 · Cited by 17

DZNep-mediated apoptosis in B-cell lymphoma is independent of the lymphoma type, EZH2 mutation status and MYC, BCL2 or BCL6 translocations

Akpa, C. A., Kleo, K., Lenze, D., Oker, E., Dimitrova, L., & Hummel, M. (2019) · PLoS ONE · doi:10.1371/journal.pone.0220681 · Cited by 17

Valproic acid upregulates the expression of the p75NTR/sortilin receptor complex to induce neuronal apoptosis

Dedoni, S., Marras, L., Olianas, M. C., Ingianni, A., & Onali, P. (2020) · APOPTOSIS · doi:10.1007/s10495-020-01626-0 · Cited by 17

High glucose-stimulated enhancer of zeste homolog-2 (EZH2) forces suppression of deptor to cause glomerular mesangial cell pathology

Das, F., Bera, A., Ghosh‐Choudhury, N., Sataranatarajan, K., Kamat, A., Kasinath, B. S., & Choudhury, G. G. (2021) · Cellular Signalling · doi:10.1016/j.cellsig.2021.110072 · Cited by 19

Delivery of EZH2-shRNA with mPEG-PEI nanoparticles for the treatment of prostate cancer in vitro

Wu, Y., Yu, J., Liu, Y.-B., YUAN, L., Yan, H., JING, J., & Xu, G. (2014) · International Journal of Molecular Medicine · doi:10.3892/ijmm.2014.1724 · Cited by 17

FOXP3 and Breast Cancer: Implications for Therapy and Diagnosis

Liu, Y., & Zheng, P. (2007) · Pharmacogenomics · doi:10.2217/14622416.8.11.1485 · Cited by 17

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