A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

Improved survival with vemurafenib in melanoma with BRAF V600E mutation

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Anaplastic Lymphoma Kinase Inhibition in Non–Small-Cell Lung Cancer

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Role of Histone H3 Lysine 27 Methylation in Polycomb-Group Silencing

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The polycomb group protein EZH2 is involved in progression of prostate cancer

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Somatic mutations altering EZH2 (Tyr641) in follicular and diffuse large B-cell lymphomas of germinal-center origin

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EZH2 is a marker of aggressive breast cancer and promotes neoplastic transformation of breast epithelial cells

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Frequent mutation of histone-modifying genes in non-Hodgkin lymphoma

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Orthogonal Regulation of Nucleophilic and Electrophilic Sites in Pd‐Catalyzed Regiodivergent Couplings between Indazoles and Isoprene

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Molecular Mechanisms of Epigenetic Regulators as Activatable Targets in Cancer Theranostics

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The Role of Histone Methyltransferases and Long Non-coding RNAs in the Regulation of T Cell Fate Decisions

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

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Treatment Approach to Newly Diagnosed Diffuse Large B-Cell Lymphoma

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Increased expression of EZH2 indicates aggressive potential of urothelial carcinoma of the bladder in a Chinese population

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

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Epigenetic control of tumor angiogenesis

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Prognostic and therapeutic value of somatic mutations in diffuse large B-cell lymphoma: A systematic review

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One-carbon metabolism in cancer: moonlighting functions of metabolic enzymes and anti-tumor therapy

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Isoform switching and exon skipping induced by the DNA methylation inhibitor 5-Aza-2′-deoxycytidine

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The Effect of Direct and Indirect EZH2 Inhibition in Rhabdomyosarcoma Cell Lines

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The pleiotropic roles of EZH2 in T-cell immunity and immunotherapy

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EZH2 inhibition or genetic ablation suppresses cyst growth in autosomal dominant polycystic kidney disease

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Beyond bevacizumab: investigating new angiogenesis inhibitors in ovarian cancer

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Transcriptional suppression of Dicer by HOXB‐AS3/EZH2 complex dictates sorafenib resistance and cancer stemness

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Dysfunction of Sister Chromatids Separation Promotes Progression of Hepatocellular Carcinoma According to Analysis of Gene Expression Profiling

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Next-generation Sequencing Discoveries in Lymphoma

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Structural assembly of Polycomb group protein and Insight of EZH2 in cancer progression

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Prostate cancer stem cell dynamics in the evolution of drug resistance

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Combination Treatment with GSK126 and Pomalidomide Induces B-Cell Differentiation in EZH2 Gain-of-Function Mutant Diffuse Large B-Cell Lymphoma

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Polycomb repressor complex: Its function in human cancer and therapeutic target strategy

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Chromatin Modulation of Herpesvirus Lytic Gene Expression: Managing Nucleosome Density and Heterochromatic Histone Modifications

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A Role for Monomethylation of Histone H3-K27 in Gene Activity inDrosophila

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Polycomb repressive complex 2 inhibitors: emerging epigenetic modulators

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Speckle-type POZ protein functions as a tumor suppressor in non-small cell lung cancer due to DNA methylation

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The Elements of Translational Chemical Biology

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Tumor-suppressive functions of protein lysine methyltransferases

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Histone Methylases as Novel Drug Targets: Developing Inhibitors of EZH2

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Recent Progress in the Discovery of Small-Molecule Inhibitors of the Hmt Ezh2 for the Treatment of Cancer

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A repressive role of enhancer of zeste homolog 2 in 11β-hydroxysteroid dehydrogenase type 2 expression in the human placenta

Zuo, R.-J., Liu, X., Wang, W., Li, W., Ying, H., & Sun, K. (2017) · Journal of Biological Chemistry · doi:10.1074/jbc.m116.765800 · Cited by 14

Origins and clinical relevance of proteoforms in pediatric malignancies

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Inhibition of Histone Methyltransferase EZH2 Suppresses Endometriotic Vesicle Development in a Rat Model of Endometriosis

Seguinot, I., Luna, N., Suárez, E., Appleyard, C. B., & Flores, I. (2020) · Reproductive Sciences · doi:10.1007/s43032-020-00257-9 · Cited by 14

YZL-51N functions as a selective inhibitor of SIRT7 by NAD+ competition to impede DNA damage repair

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Overview on Epigenetic Re-programming: A Potential Therapeutic Intervention in Triple Negative Breast Cancers

Hanif, E. A. M., & Shah, S. A. (2018) · Asian Pacific Journal of Cancer Prevention · doi:10.31557/apjcp.2018.19.12.3341 · Cited by 13

Design, synthesis, and antitumor activity of PLGA nanoparticles incorporating a discovered benzimidazole derivative as EZH2 inhibitor

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Current and Potential Epigenetic Targets in Multiple Myeloma

Pawlyn, C., Kaiser, M., Davies, F. E., & Morgan, G. J. (2014) · Epigenomics · doi:10.2217/epi.14.12 · Cited by 13

Systematic analysis of the intersection of disease mutations with protein modifications

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LATS2 Positively Regulates Polycomb Repressive Complex 2

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Dual-target EZH2 inhibitor: latest advances in medicinal chemistry

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EZH2 represses mesenchymal genes and upholds the epithelial state of breast carcinoma cells

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Epigenetic therapies - a new direction in clinical medicine

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Epstein–Barr virus-associated T/natural killer-cell lymphoproliferative disorder in children and young adults has similar molecular signature to extranodal nasal natural killer/T-cell lymphoma but shows distinctive stem cell-like phenotype

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Successful Strategies in the Discovery of Small-Molecule Epigenetic Modulators with Anticancer Potential

Bayo, J., Dalvi, M. P., & Martínez, E. D. (2015) · Future Medicinal Chemistry · doi:10.4155/fmc.15.140 · Cited by 12

Targeting oncogenic and epigenetic survival pathways in lymphoma

Leslie, L. A., & Younes, A. (2013) · Leukemia & lymphoma/Leukemia and lymphoma · doi:10.3109/10428194.2013.780288 · Cited by 12

Identification of a chemical modulator of EZH2-mediated silencing by cell-based high-throughput screening assay

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Structural diversity of the epigenetics pocketome

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Deregulation of Transcriptional Enhancers in Cancer

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Survivin prevents the polycomb repressor complex 2 from methylating histone 3 lysine 27

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5-Methoxyquinoline Derivatives as a New Class of EZH2 Inhibitors

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Myeloma Propagating Cells, Drug Resistance and Relapse

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ZLD1122, a novel EZH2 and EZH1 small molecular inhibitor, blocks H3K27 methylation and diffuse large B cell lymphoma cell growth

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Integrated bioinformatics analysis of chromatin regulator EZH2 in regulating mRNA and lncRNA expression by ChIP sequencing and RNA sequencing

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Follicular lymphoma: State‐of‐the‐art ICML workshop in Lugano 2015

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Semi-Quantitative Mass Spectrometry in AML Cells Identifies New Non-Genomic Targets of the EZH2 Methyltransferase

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Three classes of response elements for human PRC2 and MLL1/2–Trithorax complexes

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Follicular lymphoma genomics

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Discovery of epigenetic modulators targeting HDACs and EZH2 simultaneously for the treatment of hematological malignancies

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Recent Advances in enhancer of zeste homolog 2 Inhibitors: Structural insights and therapeutic applications

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Synthesis of lysine methyltransferase inhibitors

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Moving beyond rituximab, cyclophosphamide, doxorubicin, vincristine and prednisone for diffuse large B-cell lymphoma

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Investigational epigenetically targeted drugs in early phase trials for the treatment of haematological malignancies

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Emerging therapeutic targets in human acute myeloid leukemia (part 2) – bromodomain inhibition should be considered as a possible strategy for various patient subsets

Reikvam, H., Hoang, T., & Bruserud, Ø. (2015) · Expert Review of Hematology · doi:10.1586/17474086.2015.1036025 · Cited by 10

The Biological Basis of Histologic Transformation

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Putting a halt on PRC2 in pediatric glioblastoma

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The Role of Histone Methylation and Methyltransferases in Gene Regulation

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Small Molecule Inhibitors of EZH2: the Emerging Translational Landscape

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Recent Advances in Small-Molecule Modulation of Epigenetic Targets

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Design, synthesis and mechanism studies of dual EZH2/BRD4 inhibitors for cancer therapy

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Ribosomal S6 protein kinase 4 promotes resistance to EZH2 inhibitors in glioblastoma

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Mining the Epigenetic Landscape of Tissue Polarity in Search of New Targets for Cancer Therapy

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Activating mutations affecting the NF-kappa B pathway and EZH2-mediated epigenetic regulation are rare events in primary mediastinal large B-cell lymphoma.

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Recent Progress in the Discovery of Epigenetic Inhibitors for the Treatment of Cancer

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Targeting EZH2 for the treatment of hepatosplenic T-cell lymphoma

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BAHD1 serves as a critical regulator of breast cancer cell proliferation and invasion

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Catalog of genetic progression of human cancers: non-Hodgkin lymphoma

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Identification of catalytic and non‐catalytic activity inhibitors against PRC2‐EZH2 complex through multiple high‐throughput screening campaigns

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Biochemical Assay Development for Histone Methyltransferases Using a Transcreener-Based Assay for S-Adenosylhomocysteine

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EPIGENETIC MECHANISM OF REGULATION OF HOX GENES AND NEUROTRANSMITTERS VIA HORMONES AND LncRNA

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EZH2 PROTACs outperform catalytic inhibitors in prostate cancer by targeting a methylation-independent function of PRC2

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Design, synthesis, and biological evaluation of novel thieno[3,2- d ]pyrimidine derivatives as potent antitumor agents

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Chemical-genetics refines transcription factor regulatory circuits

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Is Targeted Therapy Feasible in Acute Myelogenous Leukemia?

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