Emerging Epigenetic Targets and Therapies in Cancer Medicine

High-Resolution Profiling of Histone Methylations in the Human Genome

2007 • 6,479 citations

IDH1andIDH2Mutations in Gliomas

2009 • 5,312 citations

Selective inhibition of BET bromodomains

2010 • 3,775 citations

Regulation of chromatin structure by site-specific histone H3 methyltransferases

2000 • 2,709 citations

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

2011 • 2,642 citations

Leukemic IDH1 and IDH2 Mutations Result in a Hypermethylation Phenotype, Disrupt TET2 Function, and Impair Hematopoietic Differentiation

2010 • 2,561 citations

Oncometabolite 2-Hydroxyglutarate Is a Competitive Inhibitor of α-Ketoglutarate-Dependent Dioxygenases

2011 • 2,508 citations

Recurring Mutations Found by Sequencing an Acute Myeloid Leukemia Genome

2009 • 2,156 citations

The Common Feature of Leukemia-Associated IDH1 and IDH2 Mutations Is a Neomorphic Enzyme Activity Converting α-Ketoglutarate to 2-Hydroxyglutarate

2010 • 1,866 citations

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

2011 • 1,782 citations

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

2010 • 1,593 citations

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

2003 • 1,587 citations

Suppression of inflammation by a synthetic histone mimic

2010 • 1,459 citations

UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development

2007 • 1,291 citations

Histone H3 Methylation by Set2 Directs Deacetylation of Coding Regions by Rpd3S to Suppress Spurious Intragenic Transcription

2005 • 1,286 citations

Genome-wide mapping of Polycomb target genes unravels their roles in cell fate transitions

2006 • 1,244 citations

Inactivating mutations of the histone methyltransferase gene EZH2 in myeloid disorders

2010 • 1,090 citations

Targeting MYC dependence in cancer by inhibiting BET bromodomains

2011 • 1,054 citations

EZH1 Mediates Methylation on Histone H3 Lysine 27 and Complements EZH2 in Maintaining Stem Cell Identity and Executing Pluripotency

2008 • 954 citations

IDH1 and IDH2 mutations are frequent events in central chondrosarcoma and central and periosteal chondromas but not in other mesenchymal tumours

2011 • 897 citations

Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor

2011 • 890 citations

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

2007 • 871 citations

MLL-Rearranged Leukemia Is Dependent on Aberrant H3K79 Methylation by DOT1L

2011 • 841 citations

Reversal of H3K9me2 by a Small-Molecule Inhibitor for the G9a Histone Methyltransferase

2007 • 803 citations

Somatic mutations of the histone H3K27 demethylase gene UTX in human cancer

2009 • 767 citations

Demethylation of H3K27 Regulates Polycomb Recruitment and H2A Ubiquitination

2007 • 744 citations

ALL-1 Is a Histone Methyltransferase that Assembles a Supercomplex of Proteins Involved in Transcriptional Regulation

2002 • 720 citations

Histone H3 Lysine 9 Methylation and HP1γ Are Associated with Transcription Elongation through Mammalian Chromatin

2005 • 690 citations

Transformation by the (R)-enantiomer of 2-hydroxyglutarate linked to EGLN activation

2012 • 676 citations

JMJD6 Is a Histone Arginine Demethylase

2007 • 667 citations

Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas

2010 • 652 citations

The BCL6 proto-oncogene suppresses p53 expression in germinal-centre B cells

2004 • 650 citations

The Menin Tumor Suppressor Protein Is an Essential Oncogenic Cofactor for MLL-Associated Leukemogenesis

2005 • 577 citations

DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation

2009 • 561 citations

AFF4, a Component of the ELL/P-TEFb Elongation Complex and a Shared Subunit of MLL Chimeras, Can Link Transcription Elongation to Leukemia

2010 • 541 citations

Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9

2005 • 500 citations

H3K36 Methylation Antagonizes PRC2-mediated H3K27 Methylation

2011 • 500 citations

DOT1L/KMT4 Recruitment and H3K79 Methylation Are Ubiquitously Coupled with Gene Transcription in Mammalian Cells

2008 • 481 citations

Protein methyltransferases as a target class for drug discovery

2009 • 443 citations

Arginine methylation regulates the p53 response

2008 • 443 citations

NUP98–NSD1 links H3K36 methylation to Hox-A gene activation and leukaemogenesis

2007 • 421 citations

BRD–NUT oncoproteins: a family of closely related nuclear proteins that block epithelial differentiation and maintain the growth of carcinoma cells

2007 • 402 citations

MMSET regulates histone H4K20 methylation and 53BP1 accumulation at DNA damage sites

2011 • 396 citations

Structure of the Catalytic Domain of Human DOT1L, a Non-SET Domain Nucleosomal Histone Methyltransferase

2003 • 393 citations

Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia

2012 • 392 citations

The Histone H3K79 Methyltransferase Dot1L Is Essential for Mammalian Development and Heterochromatin Structure

2008 • 369 citations

Polycomb group protein-mediated repression of transcription

2010 • 366 citations

H3K9 Histone Methyltransferase G9a Promotes Lung Cancer Invasion and Metastasis by Silencing the Cell Adhesion Molecule Ep-CAM

2010 • 358 citations

Brd4 Recruits P-TEFb to Chromosomes at Late Mitosis To Promote G₁ Gene Expression and Cell Cycle Progression

2007 • 340 citations

The MMSET histone methyl transferase switches global histone methylation and alters gene expression in t(4;14) multiple myeloma cells

2010 • 327 citations

The mixed-lineage leukemia fusion partner AF4 stimulates RNA polymerase II transcriptional elongation and mediates coordinated chromatin remodeling

2006 • 314 citations

IDH1 and IDH2 mutation studies in 1473 patients with chronic-, fibrotic- or blast-phase essential thrombocythemia, polycythemia vera or myelofibrosis

2010 • 307 citations

Histone methyltransferases in cancer

2009 • 296 citations

Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294

2009 • 292 citations

NUP98/NSD1 characterizes a novel poor prognostic group in acute myeloid leukemia with a distinct HOX gene expression pattern

2011 • 288 citations

Specific peptide interference reveals BCL6 transcriptional and oncogenic mechanisms in B-cell lymphoma cells

2004 • 284 citations

EZH2-mediated epigenetic silencing in germinal center B cells contributes to proliferation and lymphomagenesis

2010 • 277 citations

Regulation of NF-κB by NSD1/FBXL11-dependent reversible lysine methylation of p65

2009 • 263 citations

JAK2V617F-Mediated Phosphorylation of PRMT5 Downregulates Its Methyltransferase Activity and Promotes Myeloproliferation

2011 • 249 citations

Critical Residues within the BTB Domain of PLZF and Bcl-6 Modulate Interaction with Corepressors

2002 • 208 citations

Differentiation of NUT Midline Carcinoma by Epigenomic Reprogramming

2011 • 196 citations

Requirement for Dot1l in murine postnatal hematopoiesis and leukemogenesis by MLL translocation

2011 • 193 citations

Downregulation of EZH2 decreases growth of estrogen receptor-negative invasive breast carcinoma and requires BRCA1

2008 • 191 citations

NUP98 is fused to the NSD3 gene in acute myeloid leukemia associated with t(8;11)(p11.2;p15)

2002 • 188 citations

The etiology of Wolf?Hirschhorn syndrome

2005 • 183 citations

Histone H3 Lysine 79 Methyltransferase Dot1 Is Required for Immortalization by MLL Oncogenes

2010 • 175 citations

NSD3, a New SET Domain-Containing Gene, Maps to 8p12 and Is Amplified in Human Breast Cancer Cell Lines

2001 • 172 citations

BCL6-mediated repression of p53 is critical for leukemia stem cell survival in chronic myeloid leukemia

2011 • 164 citations

The Histone Methyltransferase and Putative Oncoprotein MMSET Is Overexpressed in a Large Variety of Human Tumors

2011 • 124 citations

BCL6 repression of EP300 in human diffuse large B cell lymphoma cells provides a basis for rational combinatorial therapy

2010 • 116 citations

MLL: How complex does it get?

2005 • 92 citations

ES Cell Cycle Progression and Differentiation Require the Action of the Histone Methyltransferase Dot1L

2009 • 74 citations

Role of H3K27 Demethylases Jmjd3 and UTX in Transcriptional Regulation

2010 • 56 citations

NSD1 mutations in Sotos syndrome

2005 • 50 citations

The NSD3L histone methyltransferase regulates cell cycle and cell invasion in breast cancer cells

2010 • 38 citations