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Selective gene dependencies in MYCN-amplified neuroblastoma include the core transcriptional regulatory circuitry.
Nature genetics 20180901
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Inhibition of histone H3K27 demethylases selectively modulates inflammatory phenotypes of natural killer cells.
The Journal of biological chemistry 20180216
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Inhibition of Bromodomain and Extraterminal Domain Family Proteins Ameliorates Experimental Renal Damage.
Journal of the American Society of Nephrology : JASN 20170201
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Bromodomain and Extraterminal Protein Inhibitor JQ1 Suppresses Thyroid Tumor Growth in a Mouse Model.
Clinical cancer research : an official journal of the American Association for Cancer Research 20170115
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The BET inhibitor JQ1 selectively impairs tumour response to hypoxia and downregulates CA9 and angiogenesis in triple negative breast cancer.
Oncogene 20170105
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Design and characterization of bivalent BET inhibitors.
Nature chemical biology 20161201
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The BET-Bromodomain Inhibitor JQ1 Reduces Inflammation and Tau Phosphorylation at Ser396 in the Brain of the 3xTg Model of Alzheimer's Disease.
Current Alzheimer research 20160901
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Antimyeloma activity of bromodomain inhibitors on the human myeloma cell line U266 by downregulation of MYCL.
Anti-cancer drugs 20160901
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BET Inhibition Induces Apoptosis in Aggressive B-Cell Lymphoma via Epigenetic Regulation of BCL-2 Family Members.
Molecular cancer therapeutics 20160901
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Loss of TRIM33 causes resistance to BET bromodomain inhibitors through MYC- and TGF-β-dependent mechanisms.
Proceedings of the National Academy of Sciences of the United States of America 20160802
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In Silico Analysis Guides Selection of BET Inhibitors for Triple-Negative Breast Cancer Treatment.
Molecular cancer therapeutics 20160801
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BET bromodomain inhibitors suppress EWS-FLI1-dependent transcription and the IGF1 autocrine mechanism in Ewing sarcoma.
Oncotarget 20160712
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Dual Targeting of Bromodomain and Extraterminal Domain Proteins, and WNT or MAPK Signaling, Inhibits c-MYC Expression and Proliferation of Colorectal Cancer Cells.
Molecular cancer therapeutics 20160601
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Nonselective inhibition of the epigenetic transcriptional regulator BET induces marked lymphoid and hematopoietic toxicity in mice.
Toxicology and applied pharmacology 20160601
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BET and BRAF inhibitors act synergistically against BRAF-mutant melanoma.
Cancer medicine 20160601
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Epigenetic reader BRD4 inhibition as a therapeutic strategy to suppress E2F2-cell cycle regulation circuit in liver cancer.
Oncotarget 20160531
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The Bromodomain Inhibitor JQ1 and the Histone Deacetylase Inhibitor Panobinostat Synergistically Reduce N-Myc Expression and Induce Anticancer Effects.
Clinical cancer research : an official journal of the American Association for Cancer Research 20160515
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The Bromodomain BET Inhibitor JQ1 Suppresses Tumor Angiogenesis in Models of Childhood Sarcoma.
Molecular cancer therapeutics 20160501
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BRD4 Regulates EZH2 Transcription through Upregulation of C-MYC and Represents a Novel Therapeutic Target in Bladder Cancer.
Molecular cancer therapeutics 20160501
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Keap1-Independent Regulation of Nrf2 Activity by Protein Acetylation and a BET Bromodomain Protein.
PLoS genetics 20160501
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Targeting the epigenetic readers in Ewing sarcoma inhibits the oncogenic transcription factor EWS/Fli1.
Oncotarget 20160426
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Cancer Differentiating Agent Hexamethylene Bisacetamide Inhibits BET Bromodomain Proteins.
Cancer research 20160415
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Inhibition of the acetyl lysine-binding pocket of bromodomain and extraterminal domain proteins interferes with adipogenesis.
Biochemical and biophysical research communications 20160415
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MYC regulates the antitumor immune response through CD47 and PD-L1.
Science (New York, N.Y.) 20160408
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MCM5 as a target of BET inhibitors in thyroid cancer cells.
Endocrine-related cancer 20160401
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Inhibition of MUC1-C Suppresses MYC Expression and Attenuates Malignant Growth in KRAS Mutant Lung Adenocarcinomas.
Cancer research 20160315
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The BET bromodomain inhibitor JQ1 suppresses growth of pancreatic ductal adenocarcinoma in patient-derived xenograft models.
Oncogene 20160218
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Dual mTOR inhibitor MLN0128 suppresses Merkel cell carcinoma (MCC) xenograft tumor growth.
Oncotarget 20160209
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Bromodomain and extraterminal (BET) proteins regulate biliary-driven liver regeneration.
Journal of hepatology 20160201
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CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer.
The Journal of clinical investigation 20160201
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Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer.
Nature 20160121
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Suppression of BRD4 inhibits human hepatocellular carcinoma by repressing MYC and enhancing BIM expression.
Oncotarget 20160119
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Inhibition of BRD4 suppresses tumor growth and enhances iodine uptake in thyroid cancer.
Biochemical and biophysical research communications 20160115
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Targeting the EWS-ETS transcriptional program by BET bromodomain inhibition in Ewing sarcoma.
Oncotarget 20160112
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Bromodomain and extra-terminal domain bromodomain inhibition prevents synovial inflammation via blocking IκB kinase-dependent NF-κB activation in rheumatoid fibroblast-like synoviocytes.
Rheumatology (Oxford, England) 20160101
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BET protein inhibitor JQ1 inhibits growth and modulates WNT signaling in mesenchymal stem cells.
Stem cell research & therapy 20160101
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BET Bromodomain Inhibition as a Therapeutic Strategy in Ovarian Cancer by Downregulating FoxM1.
Theranostics 20160101
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BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-Cell.
PloS one 20160101
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BET Bromodomain Suppression Inhibits VEGF-induced Angiogenesis and Vascular Permeability by Blocking VEGFR2-mediated Activation of PAK1 and eNOS.
Scientific reports 20160101
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BRD4 is a novel therapeutic target for liver fibrosis.
Proceedings of the National Academy of Sciences of the United States of America 20151222
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Therapeutic targeting of BET protein BRD4 delays murine lupus.
International immunopharmacology 20151201
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Epigenetic Readers of Lysine Acetylation Regulate Cocaine-Induced Plasticity.
The Journal of neuroscience : the official journal of the Society for Neuroscience 20151111
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The BET bromodomain inhibitor, JQ1, facilitates c-FLIP degradation and enhances TRAIL-induced apoptosis independent of BRD4 and c-Myc inhibition.
Oncotarget 20151027
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Induction of USP17 by combining BET and HDAC inhibitors in breast cancer cells.
Oncotarget 20151020
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BRD4-targeted therapy induces Myc-independent cytotoxicity in Gnaq/11-mutatant uveal melanoma cells.
Oncotarget 20151020
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EGFR Mutation Promotes Glioblastoma through Epigenome and Transcription Factor Network Remodeling.
Molecular cell 20151015
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Sensitivity of Small Cell Lung Cancer to BET Inhibition Is Mediated by Regulation of ASCL1 Gene Expression.
Molecular cancer therapeutics 20151001
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BET protein Brd4 activates transcription in neurons and BET inhibitor Jq1 blocks memory in mice.
Nature neuroscience 20151001
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Combined inhibition of BET family proteins and histone deacetylases as a potential epigenetics-based therapy for pancreatic ductal adenocarcinoma.
Nature medicine 20151001
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Complete hematologic response of early T-cell progenitor acute lymphoblastic leukemia to the γ-secretase inhibitor BMS-906024: genetic and epigenetic findings in an outlier case.
Cold Spring Harbor molecular case studies 20151001
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Inhibition of Super-Enhancer Activity in Autoinflammatory Site-Derived T Cells Reduces Disease-Associated Gene Expression.
Cell reports 20150929
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Synergistic activity of BET protein antagonist-based combinations in mantle cell lymphoma cells sensitive or resistant to ibrutinib.
Blood 20150924
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BET inhibitor resistance emerges from leukaemia stem cells.
Nature 20150924
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Transcriptional and post-transcriptional control of adipocyte differentiation by Jumonji domain-containing protein 6.
Nucleic acids research 20150918
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Bromodomain and extraterminal inhibition blocks tumor progression and promotes differentiation in neuroblastoma.
Surgery 20150901
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Imiquimod-induced psoriasis-like skin inflammation is suppressed by BET bromodomain inhibitor in mice through RORC/IL-17A pathway modulation.
Pharmacological research 20150901
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BET Inhibition Upregulates SIRT1 and Alleviates Inflammatory Responses.
Chembiochem : a European journal of chemical biology 20150901
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Bromodomain-Containing Protein 4: The Epigenetic Origin of Pulmonary Arterial Hypertension.
Circulation research 20150828
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CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.
Proceedings of the National Academy of Sciences of the United States of America 20150825
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Carbonic anhydrase IX induction defines a heterogeneous cancer cell response to hypoxia and mediates stem cell-like properties and sensitivity to HDAC inhibition.
Oncotarget 20150814
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Therapeutic targeting of BET bromodomain protein, Brd4, delays cyst growth in ADPKD.
Human molecular genetics 20150715
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Targeting chromatin binding regulation of constitutively active AR variants to overcome prostate cancer resistance to endocrine-based therapies.
Nucleic acids research 20150713
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BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells.
Oncotarget 20150710
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Synergistic induction of cell death in haematological malignancies by combined phosphoinositide-3-kinase and BET bromodomain inhibition.
British journal of haematology 20150701
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Structurally diverse c-Myc inhibitors share a common mechanism of action involving ATP depletion.
Oncotarget 20150630
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BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia.
Molecular cell 20150618
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Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.
Chemistry & biology 20150618
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A Cre-conditional MYCN-driven neuroblastoma mouse model as an improved tool for preclinical studies.
Oncogene 20150601
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Synergistic effect of JQ1 and rapamycin for treatment of human osteosarcoma.
International journal of cancer 20150501
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BET bromodomain inhibition suppresses graft-versus-host disease after allogeneic bone marrow transplantation in mice.
Blood 20150423
-
Deacetylase inhibitors repress STAT5-mediated transcription by interfering with bromodomain and extra-terminal (BET) protein function.
Nucleic acids research 20150420
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Nanog requires BRD4 to maintain murine embryonic stem cell pluripotency and is suppressed by bromodomain inhibitor JQ1 together with Lefty1.
Stem cells and development 20150401
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Inhibition of BET proteins impairs estrogen-mediated growth and transcription in breast cancers by pausing RNA polymerase advancement.
Breast cancer research and treatment 20150401
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Inhibiting STAT5 by the BET bromodomain inhibitor JQ1 disrupts human dendritic cell maturation.
Journal of immunology (Baltimore, Md. : 1950) 20150401
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[Mechanism of Notch1 Pathway in SUP-B15 Cell Apoptosis Induced by JQ1].
Zhongguo shi yan xue ye xue za zhi 20150401
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JQ1 suppresses tumor growth through downregulating LDHA in ovarian cancer.
Oncotarget 20150330
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The MZF1/c-MYC axis mediates lung adenocarcinoma progression caused by wild-type lkb1 loss.
Oncogene 20150326
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BRAD4 plays a critical role in germinal center response by regulating Bcl-6 and NF-κB activation.
Cellular immunology 20150301
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Epstein-Barr virus oncoprotein super-enhancers control B cell growth.
Cell host & microbe 20150211
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Bromodomain inhibition by JQ1 suppresses lipopolysaccharide-stimulated interleukin-6 secretion in multiple myeloma cells.
Cytokine 20150201
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Resistance to everolimus driven by epigenetic regulation of MYC in ER+ breast cancers.
Oncotarget 20150201
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An in-tumor genetic screen reveals that the BET bromodomain protein, BRD4, is a potential therapeutic target in ovarian carcinoma.
Proceedings of the National Academy of Sciences of the United States of America 20150106
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Inhibition of bromodomain proteins for the treatment of human diffuse large B-cell lymphoma.
Clinical cancer research : an official journal of the American Association for Cancer Research 20150101
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GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1.
Scientific reports 20150101
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RNA sequencing reveals distinct mechanisms underlying BET inhibitor JQ1-mediated modulation of the LPS-induced activation of BV-2 microglial cells.
Journal of neuroinflammation 20150101
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BET inhibitors induce apoptosis through a MYC independent mechanism and synergise with CDK inhibitors to kill osteosarcoma cells.
Scientific reports 20150101
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Direct and indirect targeting of MYC to treat acute myeloid leukemia.
Cancer chemotherapy and pharmacology 20150101
-
Perturbation biology nominates upstream-downstream drug combinations in RAF inhibitor resistant melanoma cells.
eLife 20150101
-
Dual transcriptome sequencing reveals resistance of TLR4 ligand-activated bone marrow-derived macrophages to inflammation mediated by the BET inhibitor JQ1.
Scientific reports 20150101
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Arsenic sulfide combined with JQ1, chemotherapy agents, or celecoxib inhibit gastric and colon cancer cell growth.
Drug design, development and therapy 20150101
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BET protein inhibitor JQ1 attenuates Myc-amplified MCC tumor growth in vivo.
Cancer research 20141201
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BRD4 assists elongation of both coding and enhancer RNAs by interacting with acetylated histones.
Nature structural & molecular biology 20141201
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Chemical biology. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes.
Science (New York, N.Y.) 20141031
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NF-κB directs dynamic super enhancer formation in inflammation and atherogenesis.
Molecular cell 20141023
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PRC2 loss amplifies Ras-driven transcription and confers sensitivity to BRD4-based therapies.
Nature 20141009
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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.
Molecular cancer therapeutics 20141001
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Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors.
Proceedings of the National Academy of Sciences of the United States of America 20140805
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'Minimalist' cyclopropene-containing photo-cross-linkers suitable for live-cell imaging and affinity-based protein labeling.
Journal of the American Chemical Society 20140716
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Inducible STAT3 NH2 terminal mono-ubiquitination promotes BRD4 complex formation to regulate apoptosis.
Cellular signalling 20140701
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BET Inhibitor JQ1 Blocks Inflammation and Bone Destruction.
Journal of dental research 20140701
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An epigenomic approach to therapy for tamoxifen-resistant breast cancer.
Cell research 20140701
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Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition.
Nature medicine 20140701
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Activation of SOX2 expression by BRD4-NUT oncogenic fusion drives neoplastic transformation in NUT midline carcinoma.
Cancer research 20140615
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Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer.
Nature 20140612
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Histone deacetylase 2 and N-Myc reduce p53 protein phosphorylation at serine 46 by repressing gene transcription of tumor protein 53-induced nuclear protein 1.
Oncotarget 20140601
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Targeting Myc in KSHV-associated primary effusion lymphoma with BET bromodomain inhibitors.
Oncogene 20140529
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Bromodomain and extraterminal proteins suppress NF-E2-related factor 2-mediated antioxidant gene expression.
Journal of immunology (Baltimore, Md. : 1950) 20140515
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MLL3 is a haploinsufficient 7q tumor suppressor in acute myeloid leukemia.
Cancer cell 20140512
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Brd4 maintains constitutively active NF-κB in cancer cells by binding to acetylated RelA.
Oncogene 20140501
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Highly active combination of BRD4 antagonist and histone deacetylase inhibitor against human acute myelogenous leukemia cells.
Molecular cancer therapeutics 20140501
-
Targeting STAT5 in hematologic malignancies through inhibition of the bromodomain and extra-terminal (BET) bromodomain protein BRD2.
Molecular cancer therapeutics 20140501
-
Inhibition of BRD4 attenuates tumor cell self-renewal and suppresses stem cell signaling in MYC driven medulloblastoma.
Oncotarget 20140501
-
Therapeutic targeting of c-Myc in T-cell acute lymphoblastic leukemia, T-ALL.
Oncotarget 20140501
-
The bromodomain protein BRD4 regulates the KEAP1/NRF2-dependent oxidative stress response.
Cell death & disease 20140401
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Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1.
The Journal of biological chemistry 20140328
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Selective inhibition of BET bromodomain epigenetic signalling interferes with the bone-associated tumour vicious cycle.
Nature communications 20140319
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The double bromodomain protein Brd2 promotes B cell expansion and mitogenesis.
Journal of leukocyte biology 20140301
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BET bromodomain inhibition of MYC-amplified medulloblastoma.
Clinical cancer research : an official journal of the American Association for Cancer Research 20140215
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c-Myc inhibition prevents leukemia initiation in mice and impairs the growth of relapsed and induction failure pediatric T-ALL cells.
Blood 20140213
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Regulation of MYC expression and differential JQ1 sensitivity in cancer cells.
PloS one 20140101
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Brd4 is essential for IL-1β-induced inflammation in human airway epithelial cells.
PloS one 20140101
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The histone deacetylase Hdac1 regulates inflammatory signalling in intestinal epithelial cells.
Journal of inflammation (London, England) 20140101
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Discovery and characterization of super-enhancer-associated dependencies in diffuse large B cell lymphoma.
Cancer cell 20131209
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Disruption of the MYC-miRNA-EZH2 loop to suppress aggressive B-cell lymphoma survival and clonogenicity.
Leukemia 20131201
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BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1.
Cancer medicine 20131201
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Efficacy of BET bromodomain inhibition in Kras-mutant non-small cell lung cancer.
Clinical cancer research : an official journal of the American Association for Cancer Research 20131115
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BET bromodomain protein inhibition is a therapeutic option for medulloblastoma.
Oncotarget 20131101
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BET acetyl-lysine binding proteins control pathological cardiac hypertrophy.
Journal of molecular and cellular cardiology 20131001
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Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.
ACS medicinal chemistry letters 20130912
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Assessment of Brd4 inhibition in idiopathic pulmonary fibrosis lung fibroblasts and in vivo models of lung fibrosis.
The American journal of pathology 20130801
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Identification of potent Yes1 kinase inhibitors using a library screening approach.
Bioorganic & medicinal chemistry letters 20130801
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Identification of a novel BET bromodomain inhibitor-sensitive, gene regulatory circuit that controls Rituximab response and tumour growth in aggressive lymphoid cancers.
EMBO molecular medicine 20130801
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BET inhibition as a single or combined therapeutic approach in primary paediatric B-precursor acute lymphoblastic leukaemia.
Blood cancer journal 20130701
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BRD4 coordinates recruitment of pause release factor P-TEFb and the pausing complex NELF/DSIF to regulate transcription elongation of interferon-stimulated genes.
Molecular and cellular biology 20130601
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The methyltransferase SMYD3 mediates the recruitment of transcriptional cofactors at the myostatin and c-Met genes and regulates skeletal muscle atrophy.
Genes & development 20130601
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Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
Journal of medicinal chemistry 20130425
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Selective inhibition of tumor oncogenes by disruption of super-enhancers.
Cell 20130411
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Inhibition of BET bromodomain targets genetically diverse glioblastoma.
Clinical cancer research : an official journal of the American Association for Cancer Research 20130401
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BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses.
Journal of immunology (Baltimore, Md. : 1950) 20130401
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Targeting MYCN in neuroblastoma by BET bromodomain inhibition.
Cancer discovery 20130301
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Androgen receptor promotes ligand-independent prostate cancer progression through c-Myc upregulation.
PloS one 20130101
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Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells.
The Journal of biological chemistry 20121214
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BET bromodomain inhibition as a novel strategy for reactivation of HIV-1.
Journal of leukocyte biology 20121201
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Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins.
Proceedings of the National Academy of Sciences of the United States of America 20121120
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Reactivation of latent HIV-1 by inhibition of BRD4.
Cell reports 20121025
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Bromodomain and extra-terminal (BET) bromodomain inhibition activate transcription via transient release of positive transcription elongation factor b (P-TEFb) from 7SK small nuclear ribonucleoprotein.
The Journal of biological chemistry 20121019
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BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia.
Blood 20121004
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Small-molecule inhibition of BRDT for male contraception.
Cell 20120817
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Cancer research: Open ambition.
Nature 20120809
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Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
Bioorganic & medicinal chemistry 20120315
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Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.
Journal of medicinal chemistry 20120126
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Targeting MYC dependence in cancer by inhibiting BET bromodomains.
Proceedings of the National Academy of Sciences of the United States of America 20111004
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BET bromodomain inhibition as a therapeutic strategy to target c-Myc.
Cell 20110916
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RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia.
Nature 20110803
-
Selective inhibition of BET bromodomains.
Nature 20101223