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Chromatin proteins and modifications as drug targets

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Epigenetics in cancer stem cells

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Methionine is a metabolic dependency of tumor-initiating cells

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Cancer mediates effector T cell dysfunction by targeting microRNAs and EZH2 via glycolysis restriction

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MeCP2 Controls an Epigenetic Pathway That Promotes Myofibroblast Transdifferentiation and Fibrosis

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Context-Specific Regulation of NF-κB Target Gene Expression by EZH2 in Breast Cancers

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Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy

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TNF/p38α/Polycomb Signaling to Pax7 Locus in Satellite Cells Links Inflammation to the Epigenetic Control of Muscle Regeneration

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Cancer Development, Progression, and Therapy: An Epigenetic Overview

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The roles of Polycomb repressive complexes in mammalian development and cancer

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Histone demethylase JMJD3 contributes to epigenetic control of <i>INK4a/ARF</i> by oncogenic RAS

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Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells

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Targeted Disruption of the EZH2/EED Complex Inhibits EZH2-dependent Cancer

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Histone lysine methylation and demethylation pathways in cancer

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Maternal diet and aging alter the epigenetic control of a promoter–enhancer interaction at the <i>Hnf4a</i> gene in rat pancreatic islets

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Targeting DNA methylation for epigenetic therapy

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Leukaemogenesis: more than mutant genes

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Molecular subtypes of breast cancer are associated with characteristic DNA methylation patterns

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Histone methyltransferases in cancer

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PRC2 directly methylates GATA4 and represses its transcriptional activityPreprint

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PML-RARα/RXR Alters the Epigenetic Landscape in Acute Promyelocytic Leukemia

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The Polycomb Protein Ezh2 Regulates Differentiation and Plasticity of CD4+ T Helper Type 1 and Type 2 Cells

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Regulation and Role of EZH2 in Cancer

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Enhancer of zeste homolog 2 epigenetically silences multiple tumor suppressor microRNAs to promote liver cancer metastasis

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Regulation of Cellular Senescence by Polycomb Chromatin Modifiers through Distinct DNA Damage- and Histone Methylation-Dependent Pathways

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PRC2 Epigenetically Silences Th1-Type Chemokines to Suppress Effector T-Cell Trafficking in Colon Cancer

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Cancer Epigenetics: Modifications, Screening, and Therapy

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Cancer DNA Methylation: Molecular Mechanisms and Clinical Implications

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EZH2 inhibition sensitizes BRG1 and EGFR mutant lung tumours to TopoII inhibitors

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MicroRNA-101 negatively regulates Ezh2 and its expression is modulated by androgen receptor and HIF-1α/HIF-1β

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EZH2 Generates a Methyl Degron that Is Recognized by the DCAF1/DDB1/CUL4 E3 Ubiquitin Ligase Complex

Lee, J. M., Lee, J. S., Kim, H.-K., Kim, K., Park, H., Kim, J.-Y., Lee, S. H., Kim, I. S., Kim, J., Lee, M., et al. (2012) · Molecular Cell · doi:10.1016/j.molcel.2012.09.004 · Cited by 250 · see citing works

Targeting Epigenetics in Cancer

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miR-449a and miR-449b are direct transcriptional targets of E2F1 and negatively regulate pRb–E2F1 activity through a feedback loop by targeting CDK6 and CDC25APreprint

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Throwing the cancer switch: reciprocal roles of polycomb and trithorax proteins

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Epigenetic Analysis of KSHV Latent and Lytic Genomes

Tóth, Z., Maglinte, D. T., Lee, S. H., Lee, H.-R., Wong, L.-Y., Brulois, K., Lee, S., Buckley, J. D., Laird, P. W., Márquez, V. E., et al. (2010) · PLoS Pathogens · doi:10.1371/journal.ppat.1001013 · Cited by 234 · see citing works

Discovery of a first-in-class EZH2 selective degrader

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miR-101 is down-regulated in glioblastoma resulting in EZH2-induced proliferation, migration, and angiogenesis

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EZH2: biology, disease, and structure-based drug discovery

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DACT3 Is an Epigenetic Regulator of Wnt/β-Catenin Signaling in Colorectal Cancer and Is a Therapeutic Target of Histone Modifications

Jiang, X., Tan, J. Y., Li, J., Kivimäe, S., Yang, X., Zhuang, L., Lee, P. L., Chan, M. T. W., Stanton, L. W., Liu, E. T., et al. (2008) · Cancer Cell · doi:10.1016/j.ccr.2008.04.019 · Cited by 235 · see citing works

Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia

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Epigenetics in Prostate Cancer: Biologic and Clinical Relevance

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FGF-2 Regulates Cell Proliferation, Migration, and Angiogenesis through an NDY1/KDM2B-miR-101-EZH2 Pathway

Kottakis, F., Polytarchou, C., Foltopoulou, P. F., Sanidas, I., Kampranis, S. C., & Tsichlis, P. N. (2011) · Molecular Cell · doi:10.1016/j.molcel.2011.06.020 · Cited by 224 · see citing works

Integrative Genomics Analysis Reveals Silencing of β-Adrenergic Signaling by Polycomb in Prostate Cancer

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The histone methyltransferase inhibitor, DZNep, up-regulates TXNIP, increases ROS production, and targets leukemia cells in AML

Zhou, J., Bi, C., Cheong, L.-L., Mahara, S., Liu, S.-C., Tay, K.-G., Koh, T.-L., Yu, Q., & Chng, W. J. (2011) · Blood · doi:10.1182/blood-2010-07-294827 · Cited by 216 · see citing works

Delivery of CRISPR/Cas systems for cancer gene therapy and immunotherapy

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Epigenetic regulation of heterochromatic DNA stability

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EZH2-Mediated Concordant Repression of Wnt Antagonists Promotes β-Catenin–Dependent Hepatocarcinogenesis

Cheng, A. S. L., Lau, S. S., Chen, Y., Kondo, Y., Li, M. S. M., Feng, H., Ching, A. K.-K., Cheung, K. F., Wong, H. K., TONG, J. H. M., et al. (2011) · Cancer Research · doi:10.1158/0008-5472.can-10-3342 · Cited by 208 · see citing works

Concise Review: Roles of Polycomb Group Proteins in Development and Disease: A Stem Cell Perspective

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Ovarian Cancer Stem Cell–Like Side Populations Are Enriched Following Chemotherapy and Overexpress EZH2

Rizzo, S., Hersey, J. M., Mellor, P., Dai, W., Santos‐Silva, A., Liber, D., Luk, L., Titley, I., Carden, C. P., Box, G., et al. (2011) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-10-0788 · Cited by 203 · see citing works

Coordinated Regulation of Polycomb Group Complexes through microRNAs in Cancer

Cao, Q., Mani, R. S., Ateeq, B., Dhanasekaran, S. M., Asangani, I. A., Prensner, J. R., Kim, J. H., Brenner, J. C., Jing, X., Cao, X., et al. (2011) · Cancer Cell · doi:10.1016/j.ccr.2011.06.016 · Cited by 204 · see citing works

Therapeutic targeting of tumor suppressor genes

Morris, L. G. T., & Chan, T. A.-T. (2014) · Cancer · doi:10.1002/cncr.29140 · Cited by 201 · see citing works

Enhancer of zeste homolog 2 (EZH2) inhibitors

Gulati, N., Béguelin, W., & Giulino-Roth, L. G. (2018) · Leukemia & lymphoma/Leukemia and lymphoma · doi:10.1080/10428194.2018.1430795 · Cited by 196 · see citing works

The H3K27me3 demethylase UTX is a gender-specific tumor suppressor in T-cell acute lymphoblastic leukemia

der Meulen, J. V., Sanghvi, V. R., Mavrakis, K. J., Durinck, K., Fang, F., Matthijssens, F., Rondou, P., Rosen, M., Pieters, T., Vandenberghe, P., et al. (2014) · Blood · doi:10.1182/blood-2014-05-577270 · Cited by 196 · see citing works

Epi-drugs to fight cancer: From chemistry to cancer treatment, the road ahead

Mai, A., & Altucci, L. (2008) · The International Journal of Biochemistry & Cell Biology · doi:10.1016/j.biocel.2008.08.020 · Cited by 190 · see citing works

Targeting histone lysine methylation in cancer

McGrath, J. P., & Trojer, P. (2015) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2015.01.002 · Cited by 188 · see citing works

Enhancer of Zeste Homolog 2 Inhibition Attenuates Renal Fibrosis by Maintaining Smad7 and Phosphatase and Tensin Homolog Expression

Zhou, X., Zang, X., Ponnusamy, M., Masucci, M. V., Tolbert, E. M., Gong, R., Zhao, T. C., Liu, N., Bayliss, G. P., Dworkin, L. D., et al. (2015) · Journal of the American Society of Nephrology · doi:10.1681/asn.2015040457 · Cited by 187 · see citing works

CRL4B Catalyzes H2AK119 Monoubiquitination and Coordinates with PRC2 to Promote Tumorigenesis

Hu, H., Yang, Y., Ji, Q., Zhao, W., Jiang, B., Liu, R., Yuan, J., Liu, Q., Li, X., Zou, Y., et al. (2012) · Cancer Cell · doi:10.1016/j.ccr.2012.10.024 · Cited by 185 · see citing works

DNMT1 and EZH2 mediated methylation silences the microRNA-200b/a/429 gene and promotes tumor progression

Ning, X., Shi, Z., Liu, X., Zhang, A., Han, L., Jiang, K., Kang, C., & Zhang, Q. (2015) · Cancer Letters · doi:10.1016/j.canlet.2015.01.005 · Cited by 186 · see citing works

STAT3 signaling drives EZH2 transcriptional activation and mediates poor prognosis in gastric cancer

Pan, Y., Wang, C., Zhu, M., Xing, R., Cui, J., Li, W.-M., Yu, D.-D., Wang, S., Zhu, W., Wu, Y., et al. (2016) · Molecular Cancer · doi:10.1186/s12943-016-0561-z · Cited by 185 · see citing works

MYC—Master Regulator of the Cancer Epigenome and Transcriptome

Poole, C. J., & van Riggelen, J. (2017) · Genes · doi:10.3390/genes8050142 · Cited by 177 · see citing works

ANRIL: A Regulator of VEGF in Diabetic Retinopathy

Thomas, A. A., Feng, B., & Chakrabarti, S. (2017) · Investigative Ophthalmology & Visual Science · doi:10.1167/iovs.16-20569 · Cited by 181 · see citing works

EZH2 negatively regulates PD-L1 expression in hepatocellular carcinoma

Xiao, G., Jin, L.-L., Liu, C., Wang, Y., Meng, Y.-M., Zhou, Z., Chen, J., Yu, X.-J., Zhang, Y., Xu, J., et al. (2019) · Journal for ImmunoTherapy of Cancer · doi:10.1186/s40425-019-0784-9 · Cited by 182 · see citing works

PRC2 overexpression and PRC2-target gene repression relating to poorer prognosis in small cell lung cancer

Sato, T., Kaneda, A., Tsuji, S., Isagawa, T., Yamamoto, S., Fujita, T., Yamanaka, R., Tanaka, Y., Nukiwa, T., Márquez, V. E., et al. (2013) · Scientific Reports · doi:10.1038/srep01911 · Cited by 177 · see citing works

EZH2 in normal and malignant hematopoiesis

Lund, K., Adams, P. D., & Copland, M. (2013) · Leukemia · doi:10.1038/leu.2013.288 · Cited by 175 · see citing works

Epigenetic mechanisms in glioblastoma multiforme

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The Impact of Chromatin Dynamics on Cas9-Mediated Genome Editing in Human Cells

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Modeling medulloblastoma in vivo and with human cerebellar organoids

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Early life stress in fathers improves behavioural flexibility in their offspring

Gapp, K., Soldado-Magraner, S., Álvarez-Sánchez, M., Bohacek, J., Vernaz, G., Shu, H., Franklin, T. B., Wolfer, D. P., & Mansuy, I. M. (2014) · Nature Communications · doi:10.1038/ncomms6466 · Cited by 170 · see citing works

EZH2 Mediates Epigenetic Silencing of Neuroblastoma Suppressor Genes CASZ1 , CLU , RUNX3 , and NGFR

Wang, C., Liu, Z., Woo, C., Li, Z., Wang, L., Wei, J. S., Márquez, V. E., Bates, S. E., Jin, Q., Khan, J. I., et al. (2011) · Cancer Research · doi:10.1158/0008-5472.can-11-0961 · Cited by 174 · see citing works

Pharmacologic disruption of Polycomb Repressive Complex 2 inhibits tumorigenicity and tumor progression in prostate cancer

Crea, F., Hurt, E. M., Mathews, L., Cabarcas‐Petroski, S., Sun, L., Márquez, V. E., Danesi, R., & Farrar, W. L. (2011) · Molecular Cancer · doi:10.1186/1476-4598-10-40 · Cited by 173 · see citing works

The emerging role of PI3K/AKT-mediated epigenetic regulation in cancer

Spangle, J. M., Roberts, T. M., & Zhao, J. J. (2017) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2017.03.002 · Cited by 169 · see citing works

Polycomb-dependent epigenetic landscape in adult T-cell leukemia

Fujikawa, D., Nakagawa, S., Hori, M., Kurokawa, N., Soejima, A., Nakano, K., Yamochi, T., Nakashima, M., Kobayashi, S., Tanaka, Y., et al. (2016) · Blood · doi:10.1182/blood-2015-08-662593 · Cited by 172 · see citing works

Oxidative Stress and DNA Methylation in Prostate Cancer

Donkena, K. V., Young, C. Y. F., & Tindall, D. J. (2010) · Obstetrics and Gynecology International · doi:10.1155/2010/302051 · Cited by 169 · see citing works

Epigenetic aberrations during oncogenesis

Hatziapostolou, M., & Iliopoulos, D. (2011) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-010-0624-z · Cited by 169 · see citing works

Roles of thioredoxin binding protein (TXNIP) in oxidative stress, apoptosis and cancer

Zhou, J., & Chng, W. J. (2012) · Mitochondrion · doi:10.1016/j.mito.2012.06.004 · Cited by 170 · see citing works

FOXQ1 Regulates Epithelial-Mesenchymal Transition in Human Cancers

Qiao, Y., Jiang, X., Lee, S. T., Karuturi, R. K. M., Hooi, S. C., & Yu, Q. (2011) · Cancer Research · doi:10.1158/0008-5472.can-10-2787 · Cited by 166 · see citing works

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 · see citing works

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 84 · see citing works

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 · see citing works