标题
Targeting BET bromodomains for cancer treatment
作者
关键词
-
出版物
Epigenomics
Volume 7, Issue 3, Pages 487-501
出版商
Future Medicine Ltd
发表日期
2015-06-16
DOI
10.2217/epi.14.91
参考文献
相关参考文献
注意:仅列出部分参考文献,下载原文获取全部文献信息。- Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia (AML)
- (2015) Harald Herrmann et al. Oncotarget
- Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer.
- (2015) Anastasia Wyce et al. Oncotarget
- BET bromodomain protein inhibition is a therapeutic option for medulloblastoma
- (2015) Anton George Henssen et al. Oncotarget
- 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
- (2015) Jeyran Shahbazi et al. Oncotarget
- Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors
- (2014) Stuart W. J. Ember et al. ACS Chemical Biology
- The bromodomain: From epigenome reader to druggable target
- (2014) Roberto Sanchez et al. Biochimica et Biophysica Acta-Gene Regulatory Mechanisms
- Disrupting the Interaction of BRD4 with Diacetylated Twist Suppresses Tumorigenesis in Basal-like Breast Cancer
- (2014) Jian Shi et al. CANCER CELL
- An epigenomic approach to therapy for tamoxifen-resistant breast cancer
- (2014) Qin Feng et al. CELL RESEARCH
- Inducible STAT3 NH2 terminal mono-ubiquitination promotes BRD4 complex formation to regulate apoptosis
- (2014) Sutapa Ray et al. CELLULAR SIGNALLING
- Privileged Diazepine Compounds and Their Emergence as Bromodomain Inhibitors
- (2014) Steven G. Smith et al. CHEMISTRY & BIOLOGY
- Selective Chemical Modulation of Gene Transcription Favors Oligodendrocyte Lineage Progression
- (2014) Mar Gacias et al. CHEMISTRY & BIOLOGY
- Bromodomains and Their Pharmacological Inhibitors
- (2014) Daniel Gallenkamp et al. ChemMedChem
- Inhibition of Bromodomain Proteins for the Treatment of Human Diffuse Large B-cell Lymphoma
- (2014) S. E. Trabucco et al. CLINICAL CANCER RESEARCH
- A mechanistic link between gene regulation and genome architecture in mammalian development
- (2014) Giancarlo Bonora et al. CURRENT OPINION IN GENETICS & DEVELOPMENT
- Chromatin: a capacitor of acetate for integrated regulation of gene expression and cell physiology
- (2014) Siavash K Kurdistani CURRENT OPINION IN GENETICS & DEVELOPMENT
- Role of Transcription Factor Acetylation in Diabetic Kidney Disease
- (2014) R. Liu et al. DIABETES
- BET bromodomain proteins are required for glioblastoma cell proliferation
- (2014) Chiara Pastori et al. Epigenetics
- Histone Cross-talk Connects Protein Phosphatase 1α (PP1α) and Histone Deacetylase (HDAC) Pathways to Regulate the Functional Transition of Bromodomain-containing 4 (BRD4) for Inducible Gene Expression
- (2014) Xiangming Hu et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Affinity Map of Bromodomain Protein 4 (BRD4) Interactions with the Histone H4 Tail and the Small Molecule Inhibitor JQ1
- (2014) Marie Jung et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- The Epigenetic Regulator I-BET151 Induces BIM-Dependent Apoptosis and Cell Cycle Arrest of Human Melanoma Cells
- (2014) Stuart J. Gallagher et al. JOURNAL OF INVESTIGATIVE DERMATOLOGY
- The Discovery of I-BET726 (GSK1324726A), a Potent Tetrahydroquinoline ApoA1 Up-Regulator and Selective BET Bromodomain Inhibitor
- (2014) Romain Gosmini et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structure-based virtual screening of novel, high-affinity BRD4 inhibitors
- (2014) Charuvaka Muvva et al. Molecular BioSystems
- BET Bromodomain Inhibitors Block Growth of Pancreatic Cancer Cells in Three-Dimensional Collagen
- (2014) V. Sahai et al. MOLECULAR CANCER THERAPEUTICS
- The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition
- (2014) Junwei Shi et al. MOLECULAR CELL
- Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer
- (2014) Irfan A. Asangani et al. NATURE
- Dual kinase-bromodomain inhibitors for rationally designed polypharmacology
- (2014) Pietro Ciceri et al. Nature Chemical Biology
- Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition
- (2014) Yujie Tang et al. NATURE MEDICINE
- Targeting bromodomains: epigenetic readers of lysine acetylation
- (2014) Panagis Filippakopoulos et al. NATURE REVIEWS DRUG DISCOVERY
- Brd4 activates P-TEFb for RNA polymerase II CTD phosphorylation
- (2014) Friederike Itzen et al. NUCLEIC ACIDS RESEARCH
- Control of NF-kB activity in human melanoma by bromodomain and extra-terminal protein inhibitor I-BET151
- (2014) Stuart J. Gallagher et al. Pigment Cell & Melanoma Research
- RVX-208, an Inducer of ApoA-I in Humans, Is a BET Bromodomain Antagonist
- (2014) Kevin G. McLure et al. PLoS One
- Regulation of MYC Expression and Differential JQ1 Sensitivity in Cancer Cells
- (2014) Trent Fowler et al. PLoS One
- BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma
- (2014) Joydeep Bhadury et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Blockade of oncogenic I B kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors
- (2014) M. Ceribelli et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes
- (2014) M. G. J. Baud et al. SCIENCE
- Design and chemoproteomic functional characterization of a chemical probe targeted to bromodomains of BET family proteins
- (2014) Jiang Wu et al. MedChemComm
- Writers and Readers of Histone Acetylation: Structure, Mechanism, and Inhibition
- (2014) R. Marmorstein et al. Cold Spring Harbor Perspectives in Biology
- The bromodomain protein BRD4 regulates the KEAP1/NRF2-dependent oxidative stress response
- (2014) M Hussong et al. Cell Death & Disease
- Bromodomain Protein BRD4 Is Required for Estrogen Receptor-Dependent Enhancer Activation and Gene Transcription
- (2014) Sankari Nagarajan et al. Cell Reports
- Driver mutations of cancer epigenomes
- (2014) David M. Roy et al. Protein & Cell
- The anticancer effects of HDAC inhibitors require the immune system
- (2014) Alison C West et al. OncoImmunology
- The Commonly Used PI3-Kinase Probe LY294002 Is an Inhibitor of BET Bromodomains
- (2013) Antje Dittmann et al. ACS Chemical Biology
- Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains
- (2013) Mathew P. Martin et al. ACS Chemical Biology
- 4-Acyl Pyrroles: Mimicking Acetylated Lysines in Histone Code Reading
- (2013) Xavier Lucas et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Histone deacetylase inhibitors
- (2013) Marije Slingerland et al. ANTI-CANCER DRUGS
- Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762
- (2013) A. Chaidos et al. BLOOD
- Discovery and Characterization of Super-Enhancer-Associated Dependencies in Diffuse Large B Cell Lymphoma
- (2013) Bjoern Chapuy et al. CANCER CELL
- PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains
- (2013) S. Picaud et al. CANCER RESEARCH
- BRD4 Sustains Melanoma Proliferation and Represents a New Target for Epigenetic Therapy
- (2013) M. F. Segura et al. CANCER RESEARCH
- Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers
- (2013) Jakob Lovén et al. CELL
- Brd4 and JMJD6-Associated Anti-Pause Enhancers in Regulation of Transcriptional Pause Release
- (2013) Wen Liu et al. CELL
- Naphthyridines as Novel BET Family Bromodomain Inhibitors
- (2013) Olivier Mirguet et al. ChemMedChem
- Efficacy of BET Bromodomain Inhibition in Kras-Mutant Non-Small Cell Lung Cancer
- (2013) T. Shimamura et al. CLINICAL CANCER RESEARCH
- Inhibition of BET Bromodomain Targets Genetically Diverse Glioblastoma
- (2013) Z. Cheng et al. CLINICAL CANCER RESEARCH
- BET Bromodomain Inhibition of MYC-Amplified Medulloblastoma
- (2013) P. Bandopadhayay et al. CLINICAL CANCER RESEARCH
- Identification of a novel BET bromodomain inhibitor-sensitive, gene regulatory circuit that controls Rituximab response and tumour growth in aggressive lymphoid cancers
- (2013) Anouk Emadali et al. EMBO Molecular Medicine
- BET bromodomain inhibitors: a patent review
- (2013) Jean-Marc Garnier et al. EXPERT OPINION ON THERAPEUTIC PATENTS
- Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains
- (2013) Olivier Mirguet et al. JOURNAL OF MEDICINAL CHEMISTRY
- Fragment-Based Drug Discovery of 2-Thiazolidinones as Inhibitors of the Histone Reader BRD4 Bromodomain
- (2013) Lele Zhao et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening
- (2013) Lewis R. Vidler et al. JOURNAL OF MEDICINAL CHEMISTRY
- [1,2,4]Triazolo[4,3-a]phthalazines: Inhibitors of Diverse Bromodomains
- (2013) Oleg Fedorov et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains
- (2013) Guangtao Zhang et al. JOURNAL OF MEDICINAL CHEMISTRY
- Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia
- (2013) M A Dawson et al. LEUKEMIA
- Phospho Switch Triggers Brd4 Chromatin Binding and Activator Recruitment for Gene-Specific Targeting
- (2013) Shwu-Yuan Wu et al. MOLECULAR CELL
- The bromodomain protein Brd4 insulates chromatin from DNA damage signalling
- (2013) Scott R. Floyd et al. NATURE
- Genome-wide localization of small molecules
- (2013) Lars Anders et al. NATURE BIOTECHNOLOGY
- MYC, a downstream target of BRD-NUT, is necessary and sufficient for the blockade of differentiation in NUT midline carcinoma
- (2013) A R Grayson et al. ONCOGENE
- Brd4 maintains constitutively active NF-κB in cancer cells by binding to acetylated RelA
- (2013) Z Zou et al. ONCOGENE
- BET Inhibition Silences Expression of MYCN and BCL2 and Induces Cytotoxicity in Neuroblastoma Tumor Models
- (2013) Anastasia Wyce et al. PLoS One
- RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain
- (2013) S. Picaud et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors
- (2013) Victor S. Gehling et al. ACS Medicinal Chemistry Letters
- BET inhibition as a single or combined therapeutic approach in primary paediatric B-precursor acute lymphoblastic leukaemia
- (2013) D Da Costa et al. Blood Cancer Journal
- Targeting MYCN in Neuroblastoma by BET Bromodomain Inhibition
- (2013) Alexandre Puissant et al. Cancer Discovery
- From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151
- (2012) Olivier Mirguet et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A)
- (2012) Jonathan Seal et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family
- (2012) Panagis Filippakopoulos et al. CELL
- Bromodomain-containing Protein 4 (BRD4) Regulates RNA Polymerase II Serine 2 Phosphorylation in Human CD4+ T Cells
- (2012) Weishi Zhang et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Bromodomain Protein Brd4 Associated with Acetylated Chromatin Is Important for Maintenance of Higher-order Chromatin Structure
- (2012) Ranran Wang et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Down-regulation of NF-κB Transcriptional Activity in HIV-associated Kidney Disease by BRD4 Inhibition
- (2012) Guangtao Zhang et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Association of bromodomain BET proteins with chromatin requires dimerization through the conserved motif B
- (2012) P. Garcia-Gutierrez et al. JOURNAL OF CELL SCIENCE
- Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit
- (2012) Paul V. Fish et al. JOURNAL OF MEDICINAL CHEMISTRY
- Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins
- (2012) W. W. Lockwood et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains
- (2012) Duncan Hay et al. MedChemComm
- A Combination of H2A.Z and H4 Acetylation Recruits Brd2 to Chromatin during Transcriptional Activation
- (2012) Ryan Draker et al. PLoS Genetics
- Pathogenesis of NUT Midline Carcinoma
- (2011) Christopher A. French Annual Review of Pathology-Mechanisms of Disease
- Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family
- (2011) Panagis Filippakopoulos et al. BIOORGANIC & MEDICINAL CHEMISTRY
- BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc
- (2011) Jake E. Delmore et al. CELL
- Real-Time Imaging of Histone H4K12–Specific Acetylation Determines the Modes of Action of Histone Deacetylase and Bromodomain Inhibitors
- (2011) Tamaki Ito et al. CHEMISTRY & BIOLOGY
- Two-pronged Binding with Bromodomain-containing Protein 4 Liberates Positive Transcription Elongation Factor b from Inactive Ribonucleoprotein Complexes
- (2011) Sebastian Schröder et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Selectivity of Kinase Inhibitor Fragments
- (2011) Paul Bamborough et al. JOURNAL OF MEDICINAL CHEMISTRY
- 3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands
- (2011) David S. Hewings et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains
- (2011) Chun-wa Chung et al. JOURNAL OF MEDICINAL CHEMISTRY
- Fragment-Based Discovery of Bromodomain Inhibitors Part 1: Inhibitor Binding Modes and Implications for Lead Discovery
- (2011) Chun-wa Chung et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structural Basis and Specificity of Acetylated Transcription Factor GATA1 Recognition by BET Family Bromodomain Protein Brd3
- (2011) R. Gamsjaeger et al. MOLECULAR AND CELLULAR BIOLOGY
- The Brd4 Extraterminal Domain Confers Transcription Activation Independent of pTEFb by Recruiting Multiple Proteins, Including NSD3
- (2011) S. Rahman et al. MOLECULAR AND CELLULAR BIOLOGY
- Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery
- (2011) Martin Philpott et al. Molecular BioSystems
- RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia
- (2011) Johannes Zuber et al. NATURE
- Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia
- (2011) Mark A. Dawson et al. NATURE
- Targeting MYC dependence in cancer by inhibiting BET bromodomains
- (2011) J. A. Mertz et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Bromodomain protein Brd3 associates with acetylated GATA1 to promote its chromatin occupancy at erythroid target genes
- (2011) J. M. Lamonica et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Oncogenesis by sequestration of CBP/p300 in transcriptionally inactive hyperacetylated chromatin domains
- (2010) Nicolas Reynoird et al. EMBO JOURNAL
- Suppression of inflammation by a synthetic histone mimic
- (2010) Edwige Nicodeme et al. NATURE
- Selective inhibition of BET bromodomains
- (2010) Panagis Filippakopoulos et al. NATURE
- Structures of the Dual Bromodomains of the P-TEFb-activating Protein Brd4 at Atomic Resolution
- (2009) Friederike Vollmuth et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Regulation of Aurora B Expression by the Bromodomain Protein Brd4
- (2009) J. You et al. MOLECULAR AND CELLULAR BIOLOGY
- The Bromodomain Protein Brd4 Stimulates G1Gene Transcription and Promotes Progression to S Phase
- (2008) Kazuki Mochizuki et al. JOURNAL OF BIOLOGICAL CHEMISTRY
Find the ideal target journal for your manuscript
Explore over 38,000 international journals covering a vast array of academic fields.
SearchBecome a Peeref-certified reviewer
The Peeref Institute provides free reviewer training that teaches the core competencies of the academic peer review process.
Get Started