Design and characterization of bivalent BET inhibitors.

Nature chemical biology 20161201

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

Antimyeloma activity of bromodomain inhibitors on the human myeloma cell line U266 by downregulation of MYCL.

Anti-cancer drugs 20160901

BET Inhibition Induces Apoptosis in Aggressive B-Cell Lymphoma via Epigenetic Regulation of BCL-2 Family Members.

Molecular cancer therapeutics 20160901

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

In Silico Analysis Guides Selection of BET Inhibitors for Triple-Negative Breast Cancer Treatment.

Molecular cancer therapeutics 20160801

BET bromodomain inhibitors suppress EWS-FLI1-dependent transcription and the IGF1 autocrine mechanism in Ewing sarcoma.

Oncotarget 20160712

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

Nonselective inhibition of the epigenetic transcriptional regulator BET induces marked lymphoid and hematopoietic toxicity in mice.

Toxicology and applied pharmacology 20160601

BET and BRAF inhibitors act synergistically against BRAF-mutant melanoma.

Cancer medicine 20160601

Epigenetic reader BRD4 inhibition as a therapeutic strategy to suppress E2F2-cell cycle regulation circuit in liver cancer.

Oncotarget 20160531

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

The Bromodomain BET Inhibitor JQ1 Suppresses Tumor Angiogenesis in Models of Childhood Sarcoma.

Molecular cancer therapeutics 20160501

BRD4 Regulates EZH2 Transcription through Upregulation of C-MYC and Represents a Novel Therapeutic Target in Bladder Cancer.

Molecular cancer therapeutics 20160501

Keap1-Independent Regulation of Nrf2 Activity by Protein Acetylation and a BET Bromodomain Protein.

PLoS genetics 20160501

Targeting the epigenetic readers in Ewing sarcoma inhibits the oncogenic transcription factor EWS/Fli1.

Oncotarget 20160426

Cancer Differentiating Agent Hexamethylene Bisacetamide Inhibits BET Bromodomain Proteins.

Cancer research 20160415

Inhibition of the acetyl lysine-binding pocket of bromodomain and extraterminal domain proteins interferes with adipogenesis.

Biochemical and biophysical research communications 20160415

MYC regulates the antitumor immune response through CD47 and PD-L1.

Science (New York, N.Y.) 20160408

MCM5 as a target of BET inhibitors in thyroid cancer cells.

Endocrine-related cancer 20160401

Inhibition of MUC1-C Suppresses MYC Expression and Attenuates Malignant Growth in KRAS Mutant Lung Adenocarcinomas.

Cancer research 20160315

The BET bromodomain inhibitor JQ1 suppresses growth of pancreatic ductal adenocarcinoma in patient-derived xenograft models.

Oncogene 20160218

Dual mTOR inhibitor MLN0128 suppresses Merkel cell carcinoma (MCC) xenograft tumor growth.

Oncotarget 20160209

Bromodomain and extraterminal (BET) proteins regulate biliary-driven liver regeneration.

Journal of hepatology 20160201

CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer.

The Journal of clinical investigation 20160201

Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer.

Nature 20160121

Suppression of BRD4 inhibits human hepatocellular carcinoma by repressing MYC and enhancing BIM expression.

Oncotarget 20160119

Inhibition of BRD4 suppresses tumor growth and enhances iodine uptake in thyroid cancer.

Biochemical and biophysical research communications 20160115

Targeting the EWS-ETS transcriptional program by BET bromodomain inhibition in Ewing sarcoma.

Oncotarget 20160112

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

BET protein inhibitor JQ1 inhibits growth and modulates WNT signaling in mesenchymal stem cells.

Stem cell research & therapy 20160101

BET Bromodomain Inhibition as a Therapeutic Strategy in Ovarian Cancer by Downregulating FoxM1.

Theranostics 20160101

BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-Cell.

PloS one 20160101

BET Bromodomain Suppression Inhibits VEGF-induced Angiogenesis and Vascular Permeability by Blocking VEGFR2-mediated Activation of PAK1 and eNOS.

Scientific reports 20160101

BRD4 is a novel therapeutic target for liver fibrosis.

Proceedings of the National Academy of Sciences of the United States of America 20151222

Therapeutic targeting of BET protein BRD4 delays murine lupus.

International immunopharmacology 20151201

Epigenetic Readers of Lysine Acetylation Regulate Cocaine-Induced Plasticity.

The Journal of neuroscience : the official journal of the Society for Neuroscience 20151111

The BET bromodomain inhibitor, JQ1, facilitates c-FLIP degradation and enhances TRAIL-induced apoptosis independent of BRD4 and c-Myc inhibition.

Oncotarget 20151027

Induction of USP17 by combining BET and HDAC inhibitors in breast cancer cells.

Oncotarget 20151020

BRD4-targeted therapy induces Myc-independent cytotoxicity in Gnaq/11-mutatant uveal melanoma cells.

Oncotarget 20151020

EGFR Mutation Promotes Glioblastoma through Epigenome and Transcription Factor Network Remodeling.

Molecular cell 20151015

Sensitivity of Small Cell Lung Cancer to BET Inhibition Is Mediated by Regulation of ASCL1 Gene Expression.

Molecular cancer therapeutics 20151001

BET protein Brd4 activates transcription in neurons and BET inhibitor Jq1 blocks memory in mice.

Nature neuroscience 20151001

Combined inhibition of BET family proteins and histone deacetylases as a potential epigenetics-based therapy for pancreatic ductal adenocarcinoma.

Nature medicine 20151001

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

Inhibition of Super-Enhancer Activity in Autoinflammatory Site-Derived T Cells Reduces Disease-Associated Gene Expression.

Cell reports 20150929

Synergistic activity of BET protein antagonist-based combinations in mantle cell lymphoma cells sensitive or resistant to ibrutinib.

Blood 20150924

BET inhibitor resistance emerges from leukaemia stem cells.

Nature 20150924

Transcriptional and post-transcriptional control of adipocyte differentiation by Jumonji domain-containing protein 6.

Nucleic acids research 20150918

Bromodomain and extraterminal inhibition blocks tumor progression and promotes differentiation in neuroblastoma.

Surgery 20150901

Imiquimod-induced psoriasis-like skin inflammation is suppressed by BET bromodomain inhibitor in mice through RORC/IL-17A pathway modulation.

Pharmacological research 20150901

BET Inhibition Upregulates SIRT1 and Alleviates Inflammatory Responses.

Chembiochem : a European journal of chemical biology 20150901

Bromodomain-Containing Protein 4: The Epigenetic Origin of Pulmonary Arterial Hypertension.

Circulation research 20150828

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

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

Therapeutic targeting of BET bromodomain protein, Brd4, delays cyst growth in ADPKD.

Human molecular genetics 20150715

Targeting chromatin binding regulation of constitutively active AR variants to overcome prostate cancer resistance to endocrine-based therapies.

Nucleic acids research 20150713

BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells.

Oncotarget 20150710

Synergistic induction of cell death in haematological malignancies by combined phosphoinositide-3-kinase and BET bromodomain inhibition.

British journal of haematology 20150701

Structurally diverse c-Myc inhibitors share a common mechanism of action involving ATP depletion.

Oncotarget 20150630

BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia.

Molecular cell 20150618

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.

Chemistry & biology 20150618

A Cre-conditional MYCN-driven neuroblastoma mouse model as an improved tool for preclinical studies.

Oncogene 20150601

Synergistic effect of JQ1 and rapamycin for treatment of human osteosarcoma.

International journal of cancer 20150501

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

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

Inhibition of BET proteins impairs estrogen-mediated growth and transcription in breast cancers by pausing RNA polymerase advancement.

Breast cancer research and treatment 20150401

Inhibiting STAT5 by the BET bromodomain inhibitor JQ1 disrupts human dendritic cell maturation.

Journal of immunology (Baltimore, Md. : 1950) 20150401

[Mechanism of Notch1 Pathway in SUP-B15 Cell Apoptosis Induced by JQ1].

Zhongguo shi yan xue ye xue za zhi 20150401

JQ1 suppresses tumor growth through downregulating LDHA in ovarian cancer.

Oncotarget 20150330

The MZF1/c-MYC axis mediates lung adenocarcinoma progression caused by wild-type lkb1 loss.

Oncogene 20150326

BRAD4 plays a critical role in germinal center response by regulating Bcl-6 and NF-κB activation.

Cellular immunology 20150301

Epstein-Barr virus oncoprotein super-enhancers control B cell growth.

Cell host & microbe 20150211

Bromodomain inhibition by JQ1 suppresses lipopolysaccharide-stimulated interleukin-6 secretion in multiple myeloma cells.

Cytokine 20150201

Resistance to everolimus driven by epigenetic regulation of MYC in ER+ breast cancers.

Oncotarget 20150201

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

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

GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1.

Scientific reports 20150101

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

BET inhibitors induce apoptosis through a MYC independent mechanism and synergise with CDK inhibitors to kill osteosarcoma cells.

Scientific reports 20150101

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

Arsenic sulfide combined with JQ1, chemotherapy agents, or celecoxib inhibit gastric and colon cancer cell growth.

Drug design, development and therapy 20150101

BET protein inhibitor JQ1 attenuates Myc-amplified MCC tumor growth in vivo.

Cancer research 20141201

BRD4 assists elongation of both coding and enhancer RNAs by interacting with acetylated histones.

Nature structural & molecular biology 20141201

Chemical biology. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes.

Science (New York, N.Y.) 20141031

NF-κB directs dynamic super enhancer formation in inflammation and atherogenesis.

Molecular cell 20141023

PRC2 loss amplifies Ras-driven transcription and confers sensitivity to BRD4-based therapies.

Nature 20141009

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

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

'Minimalist' cyclopropene-containing photo-cross-linkers suitable for live-cell imaging and affinity-based protein labeling.

Journal of the American Chemical Society 20140716

Inducible STAT3 NH2 terminal mono-ubiquitination promotes BRD4 complex formation to regulate apoptosis.

Cellular signalling 20140701

BET Inhibitor JQ1 Blocks Inflammation and Bone Destruction.

Journal of dental research 20140701

An epigenomic approach to therapy for tamoxifen-resistant breast cancer.

Cell research 20140701

Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition.

Nature medicine 20140701

Activation of SOX2 expression by BRD4-NUT oncogenic fusion drives neoplastic transformation in NUT midline carcinoma.

Cancer research 20140615

Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer.

Nature 20140612

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

Targeting Myc in KSHV-associated primary effusion lymphoma with BET bromodomain inhibitors.

Oncogene 20140529

Bromodomain and extraterminal proteins suppress NF-E2-related factor 2-mediated antioxidant gene expression.

Journal of immunology (Baltimore, Md. : 1950) 20140515

MLL3 is a haploinsufficient 7q tumor suppressor in acute myeloid leukemia.

Cancer cell 20140512

Brd4 maintains constitutively active NF-κB in cancer cells by binding to acetylated RelA.

Oncogene 20140501

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

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

Selective inhibition of BET bromodomain epigenetic signalling interferes with the bone-associated tumour vicious cycle.

Nature communications 20140319

The double bromodomain protein Brd2 promotes B cell expansion and mitogenesis.

Journal of leukocyte biology 20140301

BET bromodomain inhibition of MYC-amplified medulloblastoma.

Clinical cancer research : an official journal of the American Association for Cancer Research 20140215

c-Myc inhibition prevents leukemia initiation in mice and impairs the growth of relapsed and induction failure pediatric T-ALL cells.

Blood 20140213

Regulation of MYC expression and differential JQ1 sensitivity in cancer cells.

PloS one 20140101

Brd4 is essential for IL-1β-induced inflammation in human airway epithelial cells.

PloS one 20140101

The histone deacetylase Hdac1 regulates inflammatory signalling in intestinal epithelial cells.

Journal of inflammation (London, England) 20140101

Discovery and characterization of super-enhancer-associated dependencies in diffuse large B cell lymphoma.

Cancer cell 20131209

Disruption of the MYC-miRNA-EZH2 loop to suppress aggressive B-cell lymphoma survival and clonogenicity.

Leukemia 20131201

BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1.

Cancer medicine 20131201

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

BET bromodomain protein inhibition is a therapeutic option for medulloblastoma.

Oncotarget 20131101

BET acetyl-lysine binding proteins control pathological cardiac hypertrophy.

Journal of molecular and cellular cardiology 20131001

Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.

ACS medicinal chemistry letters 20130912

Assessment of Brd4 inhibition in idiopathic pulmonary fibrosis lung fibroblasts and in vivo models of lung fibrosis.

The American journal of pathology 20130801

Identification of potent Yes1 kinase inhibitors using a library screening approach.

Bioorganic & medicinal chemistry letters 20130801

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

BET inhibition as a single or combined therapeutic approach in primary paediatric B-precursor acute lymphoblastic leukaemia.

Blood cancer journal 20130701

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

The methyltransferase SMYD3 mediates the recruitment of transcriptional cofactors at the myostatin and c-Met genes and regulates skeletal muscle atrophy.

Genes & development 20130601

Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.

Journal of medicinal chemistry 20130425

Selective inhibition of tumor oncogenes by disruption of super-enhancers.

Cell 20130411

Inhibition of BET bromodomain targets genetically diverse glioblastoma.

Clinical cancer research : an official journal of the American Association for Cancer Research 20130401

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

Targeting MYCN in neuroblastoma by BET bromodomain inhibition.

Cancer discovery 20130301

Androgen receptor promotes ligand-independent prostate cancer progression through c-Myc upregulation.

PloS one 20130101

Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells.

The Journal of biological chemistry 20121214

BET bromodomain inhibition as a novel strategy for reactivation of HIV-1.

Journal of leukocyte biology 20121201

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

Reactivation of latent HIV-1 by inhibition of BRD4.

Cell reports 20121025

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

BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia.

Blood 20121004

Small-molecule inhibition of BRDT for male contraception.

Cell 20120817

Cancer research: Open ambition.

Nature 20120809

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.

Bioorganic & medicinal chemistry 20120315

Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.

Journal of medicinal chemistry 20120126

Targeting MYC dependence in cancer by inhibiting BET bromodomains.

Proceedings of the National Academy of Sciences of the United States of America 20111004

BET bromodomain inhibition as a therapeutic strategy to target c-Myc.

Cell 20110916

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

Nature 20110803

Selective inhibition of BET bromodomains.

Nature 20101223