Targeting bromodomains: epigenetic readers of lysine acetylation (Q28238635)

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

21 April 2017

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

21 April 2017

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Suppression of inflammation by a synthetic histone mimic

21 April 2017

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Recruitment of P-TEFb for stimulation of transcriptional elongation by the bromodomain protein Brd4

21 April 2017

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The sirtuins hst3 and Hst4p preserve genome integrity by controlling histone h3 lysine 56 deacetylation.

21 April 2017

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Chromatin modifications and their function

21 April 2017

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Translating the Histone Code

21 April 2017

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Lysine acetylation targets protein complexes and co-regulates major cellular functions

21 April 2017

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Regulation of cellular metabolism by protein lysine acetylation

21 April 2017

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brahma: a regulator of Drosophila homeotic genes structurally related to the yeast transcriptional activator SNF2/SWI2

21 April 2017

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A p300/CBP-associated factor that competes with the adenoviral oncoprotein E1A

21 April 2017

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Structure and ligand of a histone acetyltransferase bromodomain

21 April 2017

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Mammalian ASH1L is a histone methyltransferase that occupies the transcribed region of active genes

21 April 2017

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TIF1gamma, a novel member of the transcriptional intermediary factor 1 family

21 April 2017

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Structure and function of a human TAFII250 double bromodomain module

21 April 2017

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The human SWI/SNF-B chromatin-remodeling complex is related to yeast rsc and localizes at kinetochores of mitotic chromosomes

21 April 2017

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The double bromodomain-containing chromatin adaptor Brd4 and transcriptional regulation

21 April 2017

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BET domain co-regulators in obesity, inflammation and cancer

21 April 2017

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Histone recognition and large-scale structural analysis of the human bromodomain family

21 April 2017

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The structural basis for the recognition of acetylated histone H4 by the bromodomain of histone acetyltransferase gcn5p

21 April 2017

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Cooperative binding of two acetylation marks on a histone tail by a single bromodomain

21 April 2017

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A Small Molecule Binding to the Coactivator CREB-Binding Protein Blocks Apoptosis in Cardiomyocytes

21 April 2017

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Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains

21 April 2017

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Real-time imaging of histone H4K12-specific acetylation determines the modes of action of histone deacetylase and bromodomain inhibitors

21 April 2017

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Selective inhibition of BET bromodomains

21 April 2017

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Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition

21 April 2017

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BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain

21 April 2017

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Discovery and characterization of small molecule inhibitors of the BET family bromodomains

21 April 2017

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

21 April 2017

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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

21 April 2017

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

21 April 2017

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Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors

21 April 2017

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Naphthyridines as novel BET family bromodomain inhibitors

21 April 2017

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Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

21 April 2017

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Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

21 April 2017

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4-Acyl pyrroles: mimicking acetylated lysines in histone code reading

21 April 2017

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Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain

21 April 2017

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Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening

21 April 2017

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Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery

21 April 2017

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Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain

21 April 2017

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The benzodiazepine binding site of GABA A receptors as a target for the development of novel anxiolytics

21 April 2017

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Small-molecule inhibition of BRDT for male contraception

21 April 2017

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Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains

21 April 2017

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Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A)

21 April 2017

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RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

21 April 2017

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RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist

21 April 2017

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Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains

21 April 2017

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The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains

21 April 2017

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ChEMBL: a large-scale bioactivity database for drug discovery

21 April 2017

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Demystified molecular pathology of NUT midline carcinomas

21 April 2017

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Inactivating mutations of acetyltransferase genes in B-cell lymphoma

21 April 2017

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The bromodomain protein Brd4 is a positive regulatory component of P-TEFb and stimulates RNA polymerase II-dependent transcription

21 April 2017

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Bromodomain-dependent stage-specific male genome programming by Brdt

21 April 2017

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

21 April 2017

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BET Inhibition Silences Expression of MYCN and BCL2 and Induces Cytotoxicity in Neuroblastoma Tumor Models

21 April 2017

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Interchromosomal associations between alternatively expressed loci

21 April 2017

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Brd4 coactivates transcriptional activation of NF-kappaB via specific binding to acetylated RelA

21 April 2017

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Conserved P-TEFb-interacting domain of BRD4 inhibits HIV transcription

21 April 2017

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Bromodomain protein Brd4 plays a key role in Merkel cell polyomavirus DNA replication

21 April 2017

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Structural basis and specificity of acetylated transcription factor GATA1 recognition by BET family bromodomain protein Brd3

21 April 2017

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Bromodomain protein Brd3 associates with acetylated GATA1 to promote its chromatin occupancy at erythroid target genes

21 April 2017

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Anticancer activities of histone deacetylase inhibitors

21 April 2017

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

21 April 2017

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Histone H4-K16 acetylation controls chromatin structure and protein interactions

21 April 2017

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Acetylation: a regulatory modification to rival phosphorylation?

21 April 2017

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Targeting MYC dependence in cancer by inhibiting BET bromodomains

21 April 2017

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Selective inhibition of tumor oncogenes by disruption of super-enhancers

21 April 2017

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The inheritance of epigenetic defects

21 April 2017

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MLL-CBP fusion transcript in a therapy-related acute myeloid leukemia with the t(11;16)(q23;p13) which developed in an acute lymphoblastic leukemia patient with Fanconi anemia

31 March 2020

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Rubinstein-Taybi syndrome.

31 March 2020

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Histone deacetylases and cancer.

31 March 2020

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Mechanisms of resistance to histone deacetylase inhibitors

31 March 2020

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Histone deacetylases activate hepatocyte growth factor signaling by repressing microRNA-449 in hepatocellular carcinoma cells

31 March 2020

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HDAC inhibitors overcome first hurdle

31 March 2020

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HDAC inhibitor modulation of proteotoxicity as a therapeutic approach in cancer

31 March 2020

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The multi-tasking P-TEFb complex

31 March 2020

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Activation of chromatin by acetylation of histone side chains

31 March 2020

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Therapeutic application of histone deacetylase inhibitors for central nervous system disorders

31 March 2020

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Rational therapeutic combinations with histone deacetylase inhibitors for the treatment of cancer

31 March 2020

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Mixed lineage leukemia: histone H3 lysine 4 methyltransferases from yeast to human

31 March 2020

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The BRG1 transcriptional coregulator

31 March 2020

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The WSTF-SNF2h chromatin remodeling complex interacts with several nuclear proteins in transcription

31 March 2020

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Bromodomains as therapeutic targets

31 March 2020

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Place your BETs: the therapeutic potential of bromodomains

31 March 2020

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Selective small molecules blocking HIV-1 Tat and coactivator PCAF association

31 March 2020

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Target structure-based discovery of small molecules that block human p53 and CREB binding protein association

31 March 2020

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3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands

31 March 2020

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The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

31 March 2020

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In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).

31 March 2020

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[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains

31 March 2020

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Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites

31 March 2020

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Real-time imaging of histone H4 hyperacetylation in living cells

31 March 2020

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Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

31 March 2020

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Midazolam and other benzodiazepines

31 March 2020

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Clinical pharmacology, clinical efficacy, and behavioral toxicity of alprazolam: a review of the literature.

31 March 2020

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Management of prolonged seizures and status epilepticus in childhood: a systematic review

31 March 2020

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[3H]L-655,708, a novel ligand selective for the benzodiazepine site of GABAA receptors which contain the alpha 5 subunit

31 March 2020

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Identification of amino acid residues responsible for the alpha5 subunit binding selectivity of L-655,708, a benzodiazepine binding site ligand at the GABA(A) receptor

31 March 2020

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GABA(A)-receptor subtypes: clinical efficacy and selectivity of benzodiazepine site ligands.

31 March 2020

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The separation of 3H-Benzodiazepine binding sites in brain and of benzodiazepine pharmacological properties

31 March 2020

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Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors.

31 March 2020

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A novel indazolo-triazolo-benzotriazepine exerts anti-inflammatory effects by inhibition of cyclooxygenase-2 activity and nitric oxide synthase-2 expression.

31 March 2020

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Stimulation of Hepatic Apolipoprotein A-I Production by Novel Thieno-Triazolodiazepines: Roles of the Classical Benzodiazepine Receptor, PAF Receptor, and Bromodomain Binding

31 March 2020

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From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.

31 March 2020

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PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains

31 March 2020

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RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo

31 March 2020

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ApoA-I induction as a potential cardioprotective strategy: rationale for the SUSTAIN and ASSURE studies.

31 March 2020

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Novel HDL-based therapeutic agents

31 March 2020

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Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors

31 March 2020

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Pathogenesis of NUT midline carcinoma

31 March 2020

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Oncogenesis by sequestration of CBP/p300 in transcriptionally inactive hyperacetylated chromatin domains

31 March 2020

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Differentiation of NUT midline carcinoma by epigenomic reprogramming

31 March 2020

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Roles of the histone acetyltransferase monocytic leukemia zinc finger protein in normal and malignant hematopoiesis

31 March 2020

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A complex t(1;22;11)(q44;q13;q23) translocation causing MLL-p300 fusion gene in therapy-related acute myeloid leukemia

31 March 2020

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Gene expression profiling of acute myeloid leukemia with translocation t(8;16)(p11;p13) and MYST3-CREBBP rearrangement reveals a distinctive signature with a specific pattern of HOX gene expression.

31 March 2020

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Characterization of genomic breakpoints in MLL and CBP in leukemia patients with t(11;16).

31 March 2020

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31 March 2020

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Incidence and diversity of PAX5 fusion genes in childhood acute lymphoblastic leukemia.

31 March 2020

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Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762.

31 March 2020

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BET bromodomain protein inhibition is a therapeutic option for medulloblastoma.

31 March 2020

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Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML.

31 March 2020

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Highly active combination of BRD4 antagonist and histone deacetylase inhibitor against human acute myelogenous leukemia cells.

31 March 2020

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

31 March 2020

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

31 March 2020

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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

31 March 2020

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Inhibition of BET bromodomain targets genetically diverse glioblastoma

31 March 2020

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BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy

31 March 2020

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Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer

31 March 2020

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Targeting MYCN in neuroblastoma by BET bromodomain inhibition

31 March 2020

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The mechanism of transcriptional synergy of an in vitro assembled interferon-beta enhanceosome

31 March 2020

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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.

31 March 2020

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BET bromodomain proteins are required for glioblastoma cell proliferation.

31 March 2020

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

31 March 2020

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Targeting STAT5 in hematologic malignancies through inhibition of the bromodomain and extra-terminal (BET) bromodomain protein BRD2.

31 March 2020

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BET protein inhibition shows efficacy against JAK2V617F-driven neoplasms

31 March 2020

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When are the BET factors the most sensitive to bromodomain inhibitors?

31 March 2020

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

31 March 2020

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

31 March 2020

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Regulation of tissue homeostasis by NF-kappaB signalling: implications for inflammatory diseases

31 March 2020

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Control of inducible gene expression by signal-dependent transcriptional elongation

31 March 2020

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

31 March 2020

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BET bromodomain inhibition suppresses TH17-mediated pathology

31 March 2020

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Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors

31 March 2020

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Specific interaction between genotype, smoking and autoimmunity to citrullinated alpha-enolase in the etiology of rheumatoid arthritis

31 March 2020

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Brd2 disruption in mice causes severe obesity without Type 2 diabetes

31 March 2020

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BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses.

31 March 2020

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Regulation of NO synthesis, local inflammation, and innate immunity to pathogens by BET family proteins

31 March 2020

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BET bromodomains mediate transcriptional pause release in heart failure

31 March 2020

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Catalytic activity of the proteasome fine-tunes Brg1-mediated chromatin remodeling to regulate the expression of inflammatory genes

31 March 2020

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Mutations in the gene encoding the PML nuclear body protein Sp110 are associated with immunodeficiency and hepatic veno-occlusive disease

31 March 2020

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The BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation

31 March 2020

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BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism.

31 March 2020

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Interaction between cell cycle regulator, E2F-1, and NF-kappaB mediates repression of HIV-1 gene transcription

31 March 2020

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The challenge of finding a cure for HIV infection

31 March 2020

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The molecular biology of HIV latency: breaking and restoring the Tat-dependent transcriptional circuit

31 March 2020

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Recruitment of Brd4 to the human papillomavirus type 16 DNA replication complex is essential for replication of viral DNA.

31 March 2020

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Abrogation of the Brd4-positive transcription elongation factor B complex by papillomavirus E2 protein contributes to viral oncogene repression

31 March 2020

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BET proteins promote efficient murine leukemia virus integration at transcription start sites

31 March 2020

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Bromo- and extraterminal domain chromatin regulators serve as cofactors for murine leukemia virus integration

31 March 2020

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Brd2 is required for cell cycle exit and neuronal differentiation through the E2F1 pathway in mouse neuroepithelial cells.

31 March 2020

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The first bromodomain of the testis-specific double bromodomain protein Brdt is required for chromocenter organization that is modulated by genetic background

31 March 2020

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ChromoHub: a data hub for navigators of chromatin-mediated signalling

31 March 2020

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BRD4-NUT fusion oncogene: a novel mechanism in aggressive carcinoma

31 March 2020

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12 December 2020

Synthesis and biological activity of 5-phenyl-1,3,4-benzotriazepines. 25. Synthesis of (1,2,4)triazolo(4,3-a)(1,3,4)benzotriazepines and related tricyclics

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12 December 2020

Chemistry and biological activity of 1,3,4-benzotriazepines, Part 3

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12 December 2020

Growth factor requirements of childhood acute leukemia: establishment of GM-CSF-dependent cell lines

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12 December 2020