Published in Nature on October 02, 2011
Selective inhibition of tumor oncogenes by disruption of super-enhancers. Cell (2013) 8.37
Epigenetic protein families: a new frontier for drug discovery. Nat Rev Drug Discov (2012) 6.70
Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer. Nature (2014) 5.45
Histone recognition and large-scale structural analysis of the human bromodomain family. Cell (2012) 5.15
PI3K and cancer: lessons, challenges and opportunities. Nat Rev Drug Discov (2014) 4.81
Targeting bromodomains: epigenetic readers of lysine acetylation. Nat Rev Drug Discov (2014) 3.54
Small-molecule inhibition of BRDT for male contraception. Cell (2012) 3.50
DNA methylation profiling in the clinic: applications and challenges. Nat Rev Genet (2012) 3.33
Discovery and characterization of super-enhancer-associated dependencies in diffuse large B cell lymphoma. Cancer Cell (2013) 3.13
Targeting MYCN in neuroblastoma by BET bromodomain inhibition. Cancer Discov (2013) 3.11
BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia. Blood (2012) 2.91
Phospho switch triggers Brd4 chromatin binding and activator recruitment for gene-specific targeting. Mol Cell (2013) 2.83
BET domain co-regulators in obesity, inflammation and cancer. Nat Rev Cancer (2012) 2.80
Cancer stem cell definitions and terminology: the devil is in the details. Nat Rev Cancer (2012) 2.76
Chromatin proteins and modifications as drug targets. Nature (2013) 2.60
Protein arginine methyltransferases and cancer. Nat Rev Cancer (2012) 2.56
Remodeling of the enhancer landscape during macrophage activation is coupled to enhancer transcription. Mol Cell (2013) 2.55
Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins. Proc Natl Acad Sci U S A (2012) 2.52
The mechanisms behind the therapeutic activity of BET bromodomain inhibition. Mol Cell (2014) 2.47
The oncogenic BRD4-NUT chromatin regulator drives aberrant transcription within large topological domains. Genes Dev (2015) 2.28
Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat Chem Biol (2014) 2.28
Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell (2015) 2.20
Cancer-associated IDH2 mutants drive an acute myeloid leukemia that is susceptible to Brd4 inhibition. Genes Dev (2013) 2.12
Role of SWI/SNF in acute leukemia maintenance and enhancer-mediated Myc regulation. Genes Dev (2013) 2.07
MLL3 is a haploinsufficient 7q tumor suppressor in acute myeloid leukemia. Cancer Cell (2014) 1.98
Getting up to speed with transcription elongation by RNA polymerase II. Nat Rev Mol Cell Biol (2015) 1.97
BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain. Proc Natl Acad Sci U S A (2012) 1.93
Broadly neutralizing antibodies and viral inducers decrease rebound from HIV-1 latent reservoirs in humanized mice. Cell (2014) 1.91
Disrupting the interaction of BRD4 with diacetylated Twist suppresses tumorigenesis in basal-like breast cancer. Cancer Cell (2014) 1.89
Requirement for CDK6 in MLL-rearranged acute myeloid leukemia. Blood (2014) 1.89
BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism. Cell Cycle (2012) 1.88
BET inhibitor resistance emerges from leukaemia stem cells. Nature (2015) 1.88
Inhibition of BET bromodomain targets genetically diverse glioblastoma. Clin Cancer Res (2013) 1.84
Discovery of cancer drug targets by CRISPR-Cas9 screening of protein domains. Nat Biotechnol (2015) 1.83
The super elongation complex (SEC) family in transcriptional control. Nat Rev Mol Cell Biol (2012) 1.78
CDK7-Dependent Transcriptional Addiction in Triple-Negative Breast Cancer. Cell (2015) 1.77
Transcriptional plasticity promotes primary and acquired resistance to BET inhibition. Nature (2015) 1.75
An epigenetic mechanism of resistance to targeted therapy in T cell acute lymphoblastic leukemia. Nat Genet (2014) 1.74
The BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation. Nucleic Acids Res (2012) 1.73
Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol (2013) 1.72
Chemical biology. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes. Science (2014) 1.70
Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition. J Biol Chem (2012) 1.66
Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites. J Med Chem (2012) 1.64
Blockade of miR-150 maturation by MLL-fusion/MYC/LIN-28 is required for MLL-associated leukemia. Cancer Cell (2012) 1.61
Emerging targeted agents in metastatic breast cancer. Nat Rev Clin Oncol (2013) 1.59
Reawakening fetal hemoglobin: prospects for new therapies for the β-globin disorders. Blood (2012) 1.58
Autism-like syndrome is induced by pharmacological suppression of BET proteins in young mice. J Exp Med (2015) 1.58
ETV1, 4 and 5: an oncogenic subfamily of ETS transcription factors. Biochim Biophys Acta (2012) 1.58
Readout of epigenetic modifications. Annu Rev Biochem (2013) 1.57
Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. J Med Chem (2012) 1.55
Mutations in regulators of the epigenome and their connections to global chromatin patterns in cancer. Nat Rev Genet (2013) 1.53
An overview of MYC and its interactome. Cold Spring Harb Perspect Med (2014) 1.53
PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains. Cancer Res (2013) 1.53
Targeting MLL1 H3K4 methyltransferase activity in mixed-lineage leukemia. Mol Cell (2014) 1.52
Polycomb repressive complex 2 is required for MLL-AF9 leukemia. Proc Natl Acad Sci U S A (2012) 1.52
BRD4 is a novel therapeutic target for liver fibrosis. Proc Natl Acad Sci U S A (2015) 1.51
Functions of BET proteins in erythroid gene expression. Blood (2015) 1.50
The super elongation complex family of RNA polymerase II elongation factors: gene target specificity and transcriptional output. Mol Cell Biol (2012) 1.49
Transcriptional Dependencies in Diffuse Intrinsic Pontine Glioma. Cancer Cell (2017) 1.48
Genome-wide localization of small molecules. Nat Biotechnol (2013) 1.46
Perturbation biology nominates upstream-downstream drug combinations in RAF inhibitor resistant melanoma cells. Elife (2015) 1.46
BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy. Cancer Res (2013) 1.43
A novel mouse model identifies cooperating mutations and therapeutic targets critical for chronic myeloid leukemia progression. J Exp Med (2015) 1.42
A chemical probe toolbox for dissecting the cancer epigenome. Nat Rev Cancer (2017) 1.40
Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors. Proc Natl Acad Sci U S A (2012) 1.39
ENL links histone acetylation to oncogenic gene expression in acute myeloid leukaemia. Nature (2017) 1.39
Mutations in epigenetic modifiers in the pathogenesis and therapy of acute myeloid leukemia. Blood (2013) 1.37
BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia. Mol Cell (2015) 1.36
ATAC-king the complexity of SAGA during evolution. Genes Dev (2012) 1.36
RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A (2013) 1.35
The RNA Pol II elongation factor Ell3 marks enhancers in ES cells and primes future gene activation. Cell (2012) 1.33
BET bromodomain inhibition suppresses TH17-mediated pathology. J Exp Med (2013) 1.33
DNA hydroxymethylation profiling reveals that WT1 mutations result in loss of TET2 function in acute myeloid leukemia. Cell Rep (2014) 1.31
Targeting protein-protein interactions as an anticancer strategy. Trends Pharmacol Sci (2013) 1.29
An epigenomic approach to therapy for tamoxifen-resistant breast cancer. Cell Res (2014) 1.29
Discovery and development of the Polo-like kinase inhibitor volasertib in cancer therapy. Leukemia (2014) 1.28
How chemoproteomics can enable drug discovery and development. Chem Biol (2012) 1.27
Gene amplification of the histone methyltransferase SETDB1 contributes to human lung tumorigenesis. Oncogene (2013) 1.25
Recent advances in acute myeloid leukemia stem cell biology. Haematologica (2012) 1.25
Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors. Proc Natl Acad Sci U S A (2014) 1.25
An in-tumor genetic screen reveals that the BET bromodomain protein, BRD4, is a potential therapeutic target in ovarian carcinoma. Proc Natl Acad Sci U S A (2014) 1.25
BRD4 assists elongation of both coding and enhancer RNAs by interacting with acetylated histones. Nat Struct Mol Biol (2014) 1.25
Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. J Am Chem Soc (2014) 1.23
RUNX1 is a key target in t(4;11) leukemias that contributes to gene activation through an AF4-MLL complex interaction. Cell Rep (2013) 1.22
Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia. Leukemia (2013) 1.22
Kinase and BET Inhibitors Together Clamp Inhibition of PI3K Signaling and Overcome Resistance to Therapy. Cancer Cell (2015) 1.21
Transcription factor RUNX1 promotes survival of acute myeloid leukemia cells. J Clin Invest (2013) 1.20
Cancer epigenetics drug discovery and development: the challenge of hitting the mark. J Clin Invest (2014) 1.20
BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models. PLoS One (2013) 1.19
Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer. Oncotarget (2013) 1.17
Molecular landscape of acute myeloid leukemia in younger adults and its clinical relevance. Blood (2015) 1.16
Intrinsic BET inhibitor resistance in SPOP-mutated prostate cancer is mediated by BET protein stabilization and AKT-mTORC1 activation. Nat Med (2017) 1.16
Chromatin modifications as therapeutic targets in MLL-rearranged leukemia. Trends Immunol (2012) 1.15
Control of embryonic stem cell identity by BRD4-dependent transcriptional elongation of super-enhancer-associated pluripotency genes. Cell Rep (2014) 1.14
BET protein antagonist JQ1 is synergistically lethal with FLT3 tyrosine kinase inhibitor (TKI) and overcomes resistance to FLT3-TKI in AML cells expressing FLT-ITD. Mol Cancer Ther (2014) 1.13
BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells. Oncotarget (2015) 1.12
Writers and readers of histone acetylation: structure, mechanism, and inhibition. Cold Spring Harb Perspect Biol (2014) 1.12
Hijacked in cancer: the KMT2 (MLL) family of methyltransferases. Nat Rev Cancer (2015) 1.12
Bromodomain protein Brd4 plays a key role in Merkel cell polyomavirus DNA replication. PLoS Pathog (2012) 1.11
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. J Med Chem (2013) 1.09
Selective inhibition of BET bromodomains. Nature (2010) 18.79
RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia. Nature (2011) 11.44
The bromodomain protein Brd4 is a positive regulatory component of P-TEFb and stimulates RNA polymerase II-dependent transcription. Mol Cell (2005) 8.95
Recruitment of P-TEFb for stimulation of transcriptional elongation by the bromodomain protein Brd4. Mol Cell (2005) 8.92
Suppression of inflammation by a synthetic histone mimic. Nature (2010) 8.80
MLL translocations, histone modifications and leukaemia stem-cell development. Nat Rev Cancer (2007) 8.17
Cancer epigenetics reaches mainstream oncology. Nat Med (2011) 5.83
SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood (2003) 5.07
AFF4, a component of the ELL/P-TEFb elongation complex and a shared subunit of MLL chimeras, can link transcription elongation to leukemia. Mol Cell (2010) 4.99
Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes. Nat Biotechnol (2011) 4.83
JAK2 phosphorylates histone H3Y41 and excludes HP1alpha from chromatin. Nature (2009) 4.60
Hierarchical maintenance of MLL myeloid leukemia stem cells employs a transcriptional program shared with embryonic rather than adult stem cells. Cell Stem Cell (2009) 4.43
A higher-order complex containing AF4 and ENL family proteins with P-TEFb facilitates oncogenic and physiologic MLL-dependent transcription. Cancer Cell (2010) 3.47
The MMSET histone methyl transferase switches global histone methylation and alters gene expression in t(4;14) multiple myeloma cells. Blood (2010) 2.71
A Mammalian bromodomain protein, brd4, interacts with replication factor C and inhibits progression to S phase. Mol Cell Biol (2002) 2.51
The PAF complex synergizes with MLL fusion proteins at HOX loci to promote leukemogenesis. Cancer Cell (2010) 2.50
Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J Med Chem (2011) 2.45
Multiple interactions recruit MLL1 and MLL1 fusion proteins to the HOXA9 locus in leukemogenesis. Mol Cell (2010) 2.25
Conditional MLL-CBP targets GMP and models therapy-related myeloproliferative disease. EMBO J (2005) 1.79
MLL fusion proteins preferentially regulate a subset of wild-type MLL target genes in the leukemic genome. Blood (2011) 1.74
Abundant anti-apoptotic BCL-2 is a molecular target in leukaemias with t(4;11) translocation. Br J Haematol (2008) 1.24
Functional organization of the yeast proteome by systematic analysis of protein complexes. Nature (2002) 45.19
Proteome survey reveals modularity of the yeast cell machinery. Nature (2006) 20.77
Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis. Cancer Cell (2005) 17.41
Diagnosis and management of acute myeloid leukemia in adults: recommendations from an international expert panel, on behalf of the European LeukemiaNet. Blood (2009) 15.95
Active genes are tri-methylated at K4 of histone H3. Nature (2002) 15.68
Leukemic IDH1 and IDH2 mutations result in a hypermethylation phenotype, disrupt TET2 function, and impair hematopoietic differentiation. Cancer Cell (2010) 15.20
Prognostically useful gene-expression profiles in acute myeloid leukemia. N Engl J Med (2004) 11.61
Histone H3 lysine 4 methylation patterns in higher eukaryotic genes. Nat Cell Biol (2003) 8.82
Suppression of inflammation by a synthetic histone mimic. Nature (2010) 8.80
Regulation of chromatin by histone modifications. Cell Res (2011) 8.44
Cancer epigenetics: from mechanism to therapy. Cell (2012) 7.74
Methylation of histone H3 Lys 4 in coding regions of active genes. Proc Natl Acad Sci U S A (2002) 7.67
A physical and functional map of the human TNF-alpha/NF-kappa B signal transduction pathway. Nat Cell Biol (2004) 7.23
DNA methylation signatures identify biologically distinct subtypes in acute myeloid leukemia. Cancer Cell (2010) 6.72
Epigenetic protein families: a new frontier for drug discovery. Nat Rev Drug Discov (2012) 6.70
Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors. Nat Biotechnol (2007) 6.56
Human SIR2 deacetylates p53 and antagonizes PML/p53-induced cellular senescence. EMBO J (2002) 6.37
Structure of the HP1 chromodomain bound to histone H3 methylated at lysine 9. Nature (2002) 6.09
Methyltransferase recruitment and DNA hypermethylation of target promoters by an oncogenic transcription factor. Science (2002) 6.05
New nomenclature for chromatin-modifying enzymes. Cell (2007) 5.34
The Tudor domain 'Royal Family': Tudor, plant Agenet, Chromo, PWWP and MBT domains. Trends Biochem Sci (2003) 5.19
Histone deimination antagonizes arginine methylation. Cell (2004) 5.19
Candidate single-nucleotide polymorphisms from a genomewide association study of Alzheimer disease. Arch Neurol (2007) 5.09
Assessment of Minimal Residual Disease in Standard-Risk AML. N Engl J Med (2016) 5.07
Methylation of histone H4 lysine 20 controls recruitment of Crb2 to sites of DNA damage. Cell (2004) 4.99
Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes. Nat Biotechnol (2011) 4.83
Spatial distribution of di- and tri-methyl lysine 36 of histone H3 at active genes. J Biol Chem (2005) 4.78
The methyl-CpG-binding protein MeCP2 links DNA methylation to histone methylation. J Biol Chem (2002) 4.70
JAK2 phosphorylates histone H3Y41 and excludes HP1alpha from chromatin. Nature (2009) 4.60
Histone arginine methylation regulates pluripotency in the early mouse embryo. Nature (2007) 4.55
The DNA methyltransferases associate with HP1 and the SUV39H1 histone methyltransferase. Nucleic Acids Res (2003) 4.36
EMSY links the BRCA2 pathway to sporadic breast and ovarian cancer. Cell (2003) 4.33
Management of acute promyelocytic leukemia: recommendations from an expert panel on behalf of the European LeukemiaNet. Blood (2008) 4.26
An operational definition of epigenetics. Genes Dev (2009) 4.26
Human Proteinpedia enables sharing of human protein data. Nat Biotechnol (2008) 4.21
Human but not yeast CHD1 binds directly and selectively to histone H3 methylated at lysine 4 via its tandem chromodomains. J Biol Chem (2005) 4.20
A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature (2012) 4.08
Genome-wide association analysis of susceptibility and clinical phenotype in multiple sclerosis. Hum Mol Genet (2008) 3.93
The implications of alternative splicing in the ENCODE protein complement. Proc Natl Acad Sci U S A (2007) 3.93
Identification of miRNA changes in Alzheimer's disease brain and CSF yields putative biomarkers and insights into disease pathways. J Alzheimers Dis (2008) 3.84
Blimp1 associates with Prmt5 and directs histone arginine methylation in mouse germ cells. Nat Cell Biol (2006) 3.65
Induction therapy for adults with acute lymphoblastic leukemia: results of more than 1500 patients from the international ALL trial: MRC UKALL XII/ECOG E2993. Blood (2005) 3.63
Methylation of histone H3 K4 mediates association of the Isw1p ATPase with chromatin. Mol Cell (2003) 3.47
Arginine methylation at histone H3R2 controls deposition of H3K4 trimethylation. Nature (2007) 3.32
Nucleosome-interacting proteins regulated by DNA and histone methylation. Cell (2010) 3.25
Histone methylation: dynamic or static? Cell (2002) 3.12
Prediction of molecular subtypes in acute myeloid leukemia based on gene expression profiling. Haematologica (2008) 3.06
Base-pair resolution DNA methylation sequencing reveals profoundly divergent epigenetic landscapes in acute myeloid leukemia. PLoS Genet (2012) 2.94
Myc represses transcription through recruitment of DNA methyltransferase corepressor. EMBO J (2004) 2.94
Consequences of the depletion of zygotic and embryonic enhancer of zeste 2 during preimplantation mouse development. Development (2003) 2.91
Histone H3 lysine 4 methylation disrupts binding of nucleosome remodeling and deacetylase (NuRD) repressor complex. J Biol Chem (2002) 2.89
High EVI1 levels predict adverse outcome in acute myeloid leukemia: prevalence of EVI1 overexpression and chromosome 3q26 abnormalities underestimated. Blood (2008) 2.86
Targeting epigenetic readers in cancer. N Engl J Med (2012) 2.86
LRRK2 Gly2019Ser penetrance in Arab-Berber patients from Tunisia: a case-control genetic study. Lancet Neurol (2008) 2.85
Methylation at arginine 17 of histone H3 is linked to gene activation. EMBO Rep (2001) 2.83
JAK2 V617F impairs hematopoietic stem cell function in a conditional knock-in mouse model of JAK2 V617F-positive essential thrombocythemia. Blood (2010) 2.83
Unsafe SETs: histone lysine methyltransferases and cancer. Trends Biochem Sci (2002) 2.80
Selective analysis of cell-free DNA in maternal blood for evaluation of fetal trisomy. Prenat Diagn (2012) 2.79
Crosstalk between CARM1 methylation and CBP acetylation on histone H3. Curr Biol (2002) 2.78
Distinct gene expression profiles of acute myeloid/T-lymphoid leukemia with silenced CEBPA and mutations in NOTCH1. Blood (2007) 2.77
Reversing histone methylation. Nature (2005) 2.57
The SUMO E3 ligase RanBP2 promotes modification of the HDAC4 deacetylase. EMBO J (2002) 2.56
Remodeling of the enhancer landscape during macrophage activation is coupled to enhancer transcription. Mol Cell (2013) 2.55
Mutant DNMT3A: a marker of poor prognosis in acute myeloid leukemia. Blood (2012) 2.55
Orexigen-sensitive NPY/AgRP pacemaker neurons in the hypothalamic arcuate nucleus. Nat Neurosci (2004) 2.50
Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J Med Chem (2011) 2.45
Quantitative mass spectrometry in proteomics: critical review update from 2007 to the present. Anal Bioanal Chem (2012) 2.42
The oncogenic microRNA miR-22 targets the TET2 tumor suppressor to promote hematopoietic stem cell self-renewal and transformation. Cell Stem Cell (2013) 2.33
cis-acting DNA from fission yeast centromeres mediates histone H3 methylation and recruitment of silencing factors and cohesin to an ectopic site. Curr Biol (2002) 2.27
Class III phosphatidylinositol 4-kinase alpha and beta are novel host factor regulators of hepatitis C virus replication. J Virol (2009) 2.26
Prospective minimal residual disease monitoring to predict relapse of acute promyelocytic leukemia and to direct pre-emptive arsenic trioxide therapy. J Clin Oncol (2009) 2.26
Inhibition of spleen tyrosine kinase as treatment of postoperative ileus. Gut (2012) 2.20
Suppression of the antiviral response by an influenza histone mimic. Nature (2012) 2.18
Dynamic distribution of the replacement histone variant H3.3 in the mouse oocyte and preimplantation embryos. Int J Dev Biol (2006) 2.17