Chemical probes targeting epigenetic proteins: Applications beyond oncology

KATapulting toward Pluripotency and Cancer

(2017) Calley L. Hirsch et al.   JOURNAL OF MOLECULAR BIOLOGY

Monomethylated and unmethylated FUS exhibit increased binding to Transportin and distinguish FTLD-FUS from ALS-FUS

(2016) Marc Suárez-Calvet et al.   ACTA NEUROPATHOLOGICA

A Chemical Probe for the ATAD2 Bromodomain

(2016) Paul Bamborough et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Epigenetic Histone Modifications Involved in Profibrotic Gene Regulation by 12/15-Lipoxygenase and Its Oxidized Lipid Products in Diabetic Nephropathy

(2016) Hang Yuan et al.   ANTIOXIDANTS & REDOX SIGNALING

Histone H2AK119 and H2BK120 mono-ubiquitination modulate SET7/9 and SUV39H1 in type 1 diabetes-induced renal fibrosis

(2016) S. K. Goru et al.   BIOCHEMICAL JOURNAL

Bromodomains: Structure, function and pharmacology of inhibition

(2016) Elena Ferri et al.   BIOCHEMICAL PHARMACOLOGY

PRC2 and SWI/SNF Chromatin Remodeling Complexes in Health and Disease

(2016) Cigall Kadoch et al.   BIOCHEMISTRY

Super enhancers at the miR-146a and miR-155 genes contribute to self-regulation of inflammation

(2016) Qiong Duan et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

The arginine methyltransferase PRMT5 regulates CIITA-dependent MHC II transcription

(2016) Zhiwen Fan et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

S-adenosylhomocysteine induces inflammation through NFkB: A possible role for EZH2 in endothelial cell activation

(2016) Madalena Barroso et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

Methyltransferase and demethylase profiling studies during brown adipocyte differentiation

(2016) Min Jeong Son et al.   BMB Reports

Histone H4 acetylation and the epigenetic reader Brd4 are critical regulators of pluripotency in embryonic stem cells

(2016) Michelle Gonzales-Cope et al.   BMC GENOMICS

Dysregulation of protein methyltransferases in human cancer: An emerging target class for anticancer therapy

(2016) Ryuji Hamamoto et al.   CANCER SCIENCE

BRD7 plays an anti-inflammatory role during early acute inflammation by inhibiting activation of the NF-кB signaling pathway

(2016) Ran Zhao et al.   Cellular & Molecular Immunology

PDGF-BB induces PRMT1 expression through ERK1/2 dependent STAT1 activation and regulates remodeling in primary human lung fibroblasts

(2016) Qingzhu Sun et al.   CELLULAR SIGNALLING

Histone demethylases in physiology and cancer: a tale of two enzymes, JMJD3 and UTX

(2016) Kelly Marie Arcipowski et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

BET inhibitors in cancer therapeutics: a patent review

(2016) Anirban Ghoshal et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Targeting the Bromome: are we there yet?

(2016) Susanne Müller   Future Medicinal Chemistry

Deletion of Polycomb Repressive Complex 2 From Mouse Intestine Causes Loss of Stem Cells

(2016) Martijn A.J. Koppens et al.   GASTROENTEROLOGY

UTX-1 regulates Tat-induced HIV-1 transactivation via changing the methylated status of histone H3

(2016) Hong-Sheng Zhang et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition

(2016) Srimoyee Ghosh et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Inhibition of KDM6 activity during murine ESC differentiation induces DNA damage

(2016) Christine Hofstetter et al.   JOURNAL OF CELL SCIENCE

BET bromodomain inhibition enhances T cell persistence and function in adoptive immunotherapy models

(2016) Yuki Kagoya et al.   JOURNAL OF CLINICAL INVESTIGATION

BET Inhibition AttenuatesHelicobacter pylori–Induced Inflammatory Response by Suppressing Inflammatory Gene Transcription and Enhancer Activation

(2016) Jinjing Chen et al.   JOURNAL OF IMMUNOLOGY

Histone H3K27 Demethylase JMJD3 in Cooperation with NF-κB Regulates Keratinocyte Wound Healing

(2016) Jungtae Na et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6

(2016) Yudao Shen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit

(2016) Brian S. Gerstenberger et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recent Progress in Histone Demethylase Inhibitors

(2016) Tom E. McAllister et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Brd4 acetyllysine-binding protein is involved in activation of polyomavirus JC

(2016) Hassen S. Wollebo et al.   JOURNAL OF NEUROVIROLOGY

Decreased beige adipocyte number and mitochondrial respiration coincide with increased histone methyl transferase (G9a) and reduced FGF21 gene expression in Sprague–Dawley rats fed prenatal low protein and postnatal high-fat diets

(2016) Kate J. Claycombe et al.   JOURNAL OF NUTRITIONAL BIOCHEMISTRY

The Role of Protein Arginine Methyltransferases in Inflammatory Responses

(2016) Ji Hye Kim et al.   MEDIATORS OF INFLAMMATION

S6K1 Phosphorylation of H2B Mediates EZH2 Trimethylation of H3: A Determinant of Early Adipogenesis

(2016) Sang Ah Yi et al.   MOLECULAR CELL

Promoter–enhancer looping at the PPARγ2 locus during adipogenic differentiation requires the Prmt5 methyltransferase

(2016) Scott E. LeBlanc et al.   NUCLEIC ACIDS RESEARCH

Asymmetric arginine dimethylation of RelA provides a repressive mark to modulate TNFα/NF-κB response

(2016) Anja Reintjes et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Arginine methylation enhances the RNA chaperone activity of the West Nile virus host factor AUF1 p45

(2016) Susann Friedrich et al.   RNA

Pyruvate dehydrogenase kinase regulates hepatitis C virus replication

(2016) Gwon-Soo Jung et al.   Scientific Reports

Specific regulation of PRMT1 expression by PIAS1 and RKIP in BEAS-2B epithelia cells and HFL-1 fibroblasts in lung inflammation

(2016) Li Liu et al.   Scientific Reports

The H3K9 methyltransferase Setdb1 regulates TLR4-mediated inflammatory responses in macrophages

(2016) Rumi Hachiya et al.   Scientific Reports

The BET inhibitor OTX015 reactivates latent HIV-1 through P-TEFb

(2016) Panpan Lu et al.   Scientific Reports

Control of Paneth Cell Fate, Intestinal Inflammation, and Tumorigenesis by PKCλ/ι

(2016) Yuki Nakanishi et al.   Cell Reports

Transcriptomic Profiling of Extracellular RNAs Present in Cerebrospinal Fluid Identifies Differentially Expressed Transcripts in Parkinson’s Disease

(2016) Arash Hossein-nezhad et al.   Journal of Parkinsons Disease

Protein arginine methylation facilitates KCNQ channel-PIP2 interaction leading to seizure suppression

(2016) Hyun-Ji Kim et al.   eLife

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

(2016) Jude T. Deeney et al.   PLoS One

PRMT5-Mediated Methylation of NF-κB p65 at Arg174 Is Required for Endothelial CXCL11 Gene Induction in Response to TNF-α and IFN-γ Costimulation

(2016) Daniel P. Harris et al.   PLoS One

Proteomic dissection of LPS-inducible, PHF8-dependent secretome reveals novel roles of PHF8 in TLR4-induced acute inflammation and T cell proliferation

(2016) Özgün Erdoğan et al.   Scientific Reports

A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases

(2015) Mohammad S. Eram et al.   ACS Chemical Biology

CXCL8 histone H3 acetylation is dysfunctional in airway smooth muscle in asthma: regulation by BET

(2015) Rachel L. Clifford et al.   AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY

Inactivation of BRD7 results in impaired cognitive behavior and reduced synaptic plasticity of the medial prefrontal cortex

(2015) Yang Xu et al.   BEHAVIOURAL BRAIN RESEARCH

Inhibition of G9a methyltransferase stimulates fetal hemoglobin production by facilitating LCR/ -globin looping

(2015) I. Krivega et al.   BLOOD

BET bromodomain inhibition suppresses graft-versus-host disease after allogeneic bone marrow transplantation in mice

(2015) Y. Sun et al.   BLOOD

EHMT1 and EHMT2 inhibition induces fetal hemoglobin expression

(2015) A. Renneville et al.   BLOOD

The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies

(2015) Bhavatarini Vangamudi et al.   CANCER RESEARCH

Epstein-Barr Virus Oncoprotein Super-enhancers Control B Cell Growth

(2015) Hufeng Zhou et al.   Cell Host & Microbe

Histone methylation modifiers in cellular signaling pathways

(2015) Hunain Alam et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

BET Inhibition Upregulates SIRT1 and Alleviates Inflammatory Responses

(2015) Tarja Kokkola et al.   CHEMBIOCHEM

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Glucose-induced expression of the homeotic transcription factor Prep1 is associated with histone post-translational modifications in skeletal muscle

(2015) Marco Ciccarelli et al.   DIABETOLOGIA

Leveraging Cancer Therapeutics for the HIV Cure Agenda: Current Status and Future Directions

(2015) Mark N. Polizzotto et al.   DRUGS

Histone demethylases in chromatin biology and beyond

(2015) E. Dimitrova et al.   EMBO REPORTS

Open access chemical probes for epigenetic targets

(2015) Peter J Brown et al.   Future Medicinal Chemistry

Targeting bromodomain-containing protein 4 (BRD4) benefits rheumatoid arthritis

(2015) Qing-gang Zhang et al.   IMMUNOLOGY LETTERS

Therapeutic targeting of BET protein BRD4 delays murine lupus

(2015) Shitong Wei et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Transcriptional Activity of the Islet β Cell Factor Pdx1 Is Augmented by Lysine Methylation Catalyzed by the Methyltransferase Set7/9

(2015) Aarthi V. Maganti et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Histone Methyltransferase Smyd2 Is a Negative Regulator of Macrophage Activation by Suppressing Interleukin 6 (IL-6) and Tumor Necrosis Factor α (TNF-α) Production

(2015) Guiliang Xu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Set7 Facilitates Hepatitis C Virus Replication via Enzymatic Activity–Dependent Attenuation of the IFN-Related Pathway

(2015) Tao Han et al.   JOURNAL OF IMMUNOLOGY

Inhibiting STAT5 by the BET Bromodomain Inhibitor JQ1 Disrupts Human Dendritic Cell Maturation

(2015) Patricia A. Toniolo et al.   JOURNAL OF IMMUNOLOGY

PRMT1 Upregulated by Epithelial Proinflammatory Cytokines Participates in COX2 Expression in Fibroblasts and Chronic Antigen-Induced Pulmonary Inflammation

(2015) Qingzhu Sun et al.   JOURNAL OF IMMUNOLOGY

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition

(2015) Natalie H. Theodoulou et al.   JOURNAL OF MEDICINAL CHEMISTRY

H3K27 Demethylation at the Proviral Promoter Sensitizes Latent HIV to the Effects of Vorinostat inEx VivoCultures of Resting CD4+T Cells

(2015) Manoj K. Tripathy et al.   JOURNAL OF VIROLOGY

pUL69 of Human Cytomegalovirus Recruits the Cellular Protein Arginine Methyltransferase 6 via a Domain That Is Crucial for mRNA Export and Efficient Viral Replication

(2015) Marco Thomas et al.   JOURNAL OF VIROLOGY

Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation

(2015) Huw D Lewis et al.   Nature Chemical Biology

The promise and peril of chemical probes

(2015) Cheryl H Arrowsmith et al.   Nature Chemical Biology

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

(2015) Erica Korb et al.   NATURE NEUROSCIENCE

Immune attack: the role of inflammation in Alzheimer disease

(2015) Frank L. Heppner et al.   NATURE REVIEWS NEUROSCIENCE

The Epigenetic Reader BRD2 as a Specific Modulator of PAI-1 Expression in Lipopolysaccharide-Stimulated Mouse Primary Astrocytes

(2015) Chang Soon Choi et al.   NEUROCHEMICAL RESEARCH

Protein Arginine Methyltransferase 6 Enhances Polyglutamine-Expanded Androgen Receptor Function and Toxicity in Spinal and Bulbar Muscular Atrophy

(2015) Chiara Scaramuzzino et al.   NEURON

Repression of hypoxia-inducible factor α signaling by Set7-mediated methylation

(2015) Xing Liu et al.   NUCLEIC ACIDS RESEARCH

PRMT1 and PRMT4 Regulate Oxidative Stress-Induced Retinal Pigment Epithelial Cell Damage in SIRT1-Dependent and SIRT1-Independent Manners

(2015) Dong-Il Kim et al.   Oxidative Medicine and Cellular Longevity

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

(2015) Ahmed Nadeem et al.   PHARMACOLOGICAL RESEARCH

Brd4 bridges the transcriptional regulators, Aire and P-TEFb, to promote elongation of peripheral-tissue antigen transcripts in thymic stromal cells

(2015) Hideyuki Yoshida et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Long noncoding RNA derived from CD244 signaling epigenetically controls CD8+T-cell immune responses in tuberculosis infection

(2015) Yang Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses

(2015) Ariane Hammitzsch et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Bromodomain and extra-terminal domain bromodomain inhibition prevents synovial inflammation via blocking IκB kinase–dependent NF-κB activation in rheumatoid fibroblast-like synoviocytes

(2015) Youjun Xiao et al.   RHEUMATOLOGY

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

DOT1L Activity Promotes Proliferation and Protects Cortical Neural Stem Cells from Activation of ATF4-DDIT3-Mediated ER Stress In Vitro

(2015) Deborah Roidl et al.   STEM CELLS

A Subset of Human Bromodomains Recognizes Butyryllysine and Crotonyllysine Histone Peptide Modifications

(2015) E. Megan Flynn et al.   STRUCTURE

The histone H3 lysine-27 demethylase Jmjd3 plays a critical role in specific regulation of Th17 cell differentiation

(2015) Zhi Liu et al.   Journal of Molecular Cell Biology

Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound

(2015) Lorna H. Mitchell et al.   ACS Medicinal Chemistry Letters

Targeting BET bromodomains for cancer treatment

(2015) Marie Jung et al.   Epigenomics

Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery

(2015) Lei-lei Fu et al.   Oncotarget

EZH2 is crucial for both differentiation of regulatory T cells and T effector cell expansion

(2015) Xiang-Ping Yang et al.   Scientific Reports

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

(2015) Janneke G.C. Peeters et al.   Cell Reports

An In-Depth Comparison of Latency-Reversing Agent Combinations in Various In Vitro and Ex Vivo HIV-1 Latency Models Identified Bryostatin-1+JQ1 and Ingenol-B+JQ1 to Potently Reactivate Viral Gene Expression

(2015) Gilles Darcis et al.   PLoS Pathogens

Synergistic Reactivation of Latent HIV Expression by Ingenol-3-Angelate, PEP005, Targeted NF-kB Signaling in Combination with JQ1 Induced p-TEFb Activation

(2015) Guochun Jiang et al.   PLoS Pathogens

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance

(2015) O. Fedorov et al.   Science Advances

Inhibition of H3K27me3-Specific Histone Demethylases JMJD3 and UTX Blocks Reactivation of Herpes Simplex Virus 1 in Trigeminal Ganglion Neurons

(2015) Harald G. P. Messer et al.   JOURNAL OF VIROLOGY

Histone Demethylation Maintains Prdm14 and Tsix Expression and Represses Xist in Embryonic Stem Cells

(2015) Yasunao F. Kamikawa et al.   PLoS One

Transcriptomic Profiling and H3K27me3 Distribution Reveal Both Demethylase-Dependent and Independent Regulation of Developmental Gene Transcription in Cell Differentiation

(2015) Sung Chul Kang et al.   PLoS One

The TrxG Complex Mediates Cytokine Induced De Novo Enhancer Formation in Islets

(2015) Bryan R. Tennant et al.   PLoS One

The Role of H3K4me3 in Transcriptional Regulation Is Altered in Huntington’s Disease

(2015) Xianjun Dong et al.   PLoS One

Epigenetic Heterogeneity in HIV-1 Latency Establishment

(2015) Yuka Matsuda et al.   Scientific Reports

Reactivation of HIV latency by a newly modified Ingenol derivative via protein kinase Cδ–NF-κB signaling

(2014) Guochun Jiang et al.   AIDS

Epigenetic drugs against cancer: an evolving landscape

(2014) Antonella Di Costanzo et al.   ARCHIVES OF TOXICOLOGY

BET bromodomain inhibitors—A novel epigenetic approach in castration-resistant prostate cancer

(2014) Sarah E Lochrin et al.   CANCER BIOLOGY & THERAPY

Adverse Epigenetic Signatures by Histone Methyltransferase Set7 Contribute to Vascular Dysfunction in Patients With Type 2 Diabetes MellitusCLINICAL PERSPECTIVE

(2014) Francesco Paneni et al.   Circulation-Cardiovascular Genetics

Role of LDB1 in the transition from chromatin looping to transcription activation

(2014) I. Krivega et al.   GENES & DEVELOPMENT

Cytoplasmic sequestration of FUS/TLS associated with ALS alters histone marks through loss of nuclear protein arginine methyltransferase 1

(2014) Michael Tibshirani et al.   HUMAN MOLECULAR GENETICS

Methyltransferase G9A regulates T cell differentiation during murine intestinal inflammation

(2014) Frann Antignano et al.   JOURNAL OF CLINICAL INVESTIGATION

BET Inhibitor JQ1 Blocks Inflammation and Bone Destruction

(2014) S. Meng et al.   JOURNAL OF DENTAL RESEARCH

Thioredoxin-interacting protein mediates hepatic lipogenesis and inflammation via PRMT1 and PGC-1α regulation in vitro and in vivo

(2014) Min-Jung Park et al.   JOURNAL OF HEPATOLOGY

NF-κB Directs Dynamic Super Enhancer Formation in Inflammation and Atherogenesis

(2014) Jonathan D. Brown et al.   MOLECULAR CELL

The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

(2014) Junwei Shi et al.   MOLECULAR CELL

Kruidenier et al. reply

(2014) Laurens Kruidenier et al.   NATURE

Targeting bromodomains: epigenetic readers of lysine acetylation

(2014) Panagis Filippakopoulos et al.   NATURE REVIEWS DRUG DISCOVERY

A gain-of-function mouse model identifies PRMT6 as a NF-κB coactivator

(2014) Alessandra Di Lorenzo et al.   NUCLEIC ACIDS RESEARCH

Phosphorylation of HPV-16 E2 at Serine 243 Enables Binding to Brd4 and Mitotic Chromosomes

(2014) Szu-Wei Chang et al.   PLoS One

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells

(2014) D. Barsyte-Lovejoy et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Cellular Bromodomain Protein Brd4 has Multiple Functions in E2-Mediated Papillomavirus Transcription Activation

(2014) Christine Helfer et al.   Viruses-Basel

Assessment of Brd4 Inhibition in Idiopathic Pulmonary Fibrosis Lung Fibroblasts and in Vivo Models of Lung Fibrosis

(2013) Xiaoyan Tang et al.   AMERICAN JOURNAL OF PATHOLOGY

Transcriptional Control by NF-κB: Elongation in Focus

(2013) Gil Diamant et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

Single-Cell Dynamics of Genome-Nuclear Lamina Interactions

(2013) Jop Kind et al.   CELL

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

(2013) Daniela Boehm et al.   CELL CYCLE

BET bromodomain inhibition suppresses TH17-mediated pathology

(2013) Deanna A. Mele et al.   JOURNAL OF EXPERIMENTAL MEDICINE

BET Protein Function Is Required for Inflammation: Brd2 Genetic Disruption and BET Inhibitor JQ1 Impair Mouse Macrophage Inflammatory Responses

(2013) A. C. Belkina et al.   JOURNAL OF IMMUNOLOGY

Bromo- and Extraterminal Domain Chromatin Regulators Serve as Cofactors for Murine Leukemia Virus Integration

(2013) Saumya Shree Gupta et al.   JOURNAL OF VIROLOGY

Recruitment of Brd4 to the Human Papillomavirus Type 16 DNA Replication Complex Is Essential for Replication of Viral DNA

(2013) X. Wang et al.   JOURNAL OF VIROLOGY

Phospho Switch Triggers Brd4 Chromatin Binding and Activator Recruitment for Gene-Specific Targeting

(2013) Shwu-Yuan Wu et al.   MOLECULAR CELL

Lysine-specific demethylase 1 is a therapeutic target for fetal hemoglobin induction

(2013) Lihong Shi et al.   NATURE MEDICINE

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

(2013) Z Zou et al.   ONCOGENE

BRD4 Short Isoform Interacts with RRP1B, SIPA1 and Components of the LINC Complex at the Inner Face of the Nuclear Membrane

(2013) Jude Alsarraj et al.   PLoS One

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

(2013) A. Sharma et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

PRMT5 dimethylates R30 of the p65 subunit to activate NF- B

(2013) H. Wei et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Corepressor-dependent silencing of fetal hemoglobin expression by BCL11A

(2013) J. Xu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Oral Treatment Targeting the Unfolded Protein Response Prevents Neurodegeneration and Clinical Disease in Prion-Infected Mice

(2013) J. A. Moreno et al.   Science Translational Medicine

Overexpression of PRMT6 does not suppress HIV-1 Tat transactivation in cells naturally lacking PRMT6

(2013) Haran Sivakumaran et al.   Virology Journal

Lost in Transcription: Molecular Mechanisms that Control HIV Latency

(2013) Ran Taube et al.   Viruses-Basel

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

(2012) Panagis Filippakopoulos et al.   CELL

Epigenetic Chemical Probes

(2012) S Müller et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Mutations in DNMT1 cause autosomal dominant cerebellar ataxia, deafness and narcolepsy

(2012) Juliane Winkelmann et al.   HUMAN MOLECULAR GENETICS

Upregulated Protein Arginine Methyltransferase 1 by IL-4 Increases Eotaxin-1 Expression in Airway Epithelial Cells and Participates in Antigen-Induced Pulmonary Inflammation in Rats

(2012) Q. Sun et al.   JOURNAL OF IMMUNOLOGY

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

(2012) Camellia Banerjee et al.   JOURNAL OF LEUKOCYTE BIOLOGY

Control of Proinflammatory Gene Programs by Regulated Trimethylation and Demethylation of Histone H4K20

(2012) Joshua D. Stender et al.   MOLECULAR CELL

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response

(2012) Laurens Kruidenier et al.   NATURE

A miR-19 regulon that controls NF-κB signaling

(2012) Michael P. Gantier et al.   NUCLEIC ACIDS RESEARCH

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

(2012) H. S. Bandukwala et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

(2012) Sharad K. Verma et al.   ACS Medicinal Chemistry Letters

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

(2012) Wenyu Yu et al.   Nature Communications

Bromodomain Protein Brd4 Plays a Key Role in Merkel Cell Polyomavirus DNA Replication

(2012) Xin Wang et al.   PLoS Pathogens

Barrier-to-Autointegration Factor influences specific histone modifications

(2012) Rocío Montes de Oca et al.   Nucleus

Cyclin-dependent Kinase 1 (CDK1)-mediated Phosphorylation of Enhancer of Zeste 2 (Ezh2) Regulates Its Stability

(2011) Susan C. Wu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Epigenetic Silencing of HIV-1 by the Histone H3 Lysine 27 Methyltransferase Enhancer of Zeste 2

(2011) J. Friedman et al.   JOURNAL OF VIROLOGY

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

(2011) Martin Philpott et al.   Molecular BioSystems

Getting pharmaceutical R&D back on target

(2011) Mark E Bunnage   Nature Chemical Biology

A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells

(2011) Masoud Vedadi et al.   Nature Chemical Biology

Mutations in DNMT1 cause hereditary sensory neuropathy with dementia and hearing loss

(2011) Christopher J Klein et al.   NATURE GENETICS

RNA Polymerase II Stalling Promotes Nucleosome Occlusion and pTEFb Recruitment to Drive Immortalization by Epstein-Barr Virus

(2011) Richard D. Palermo et al.   PLoS Pathogens

Identification of a PRMT5-dependent repressor complex linked to silencing of human fetal globin gene expression

(2010) G. Rank et al.   BLOOD

Involvement of Histone H3 Lysine 9 (H3K9) Methyltransferase G9a in the Maintenance of HIV-1 Latency and Its Reactivation by BIX01294

(2010) Kenichi Imai et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Activating and inhibitory functions for the histone lysine methyltransferase G9a in T helper cell differentiation and function

(2010) Bernhard Lehnertz et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

The art of the chemical probe

(2010) Stephen V Frye   Nature Chemical Biology

Lysine methylation of the NF-κB subunit RelA by SETD6 couples activity of the histone methyltransferase GLP at chromatin to tonic repression of NF-κB signaling

(2010) Dan Levy et al.   NATURE IMMUNOLOGY

Chemical genetic strategy identifies histone deacetylase 1 (HDAC1) and HDAC2 as therapeutic targets in sickle cell disease

(2010) James E. Bradner et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Brd2disruption in mice causes severe obesity without Type 2 diabetes

(2009) Fangnian Wang et al.   BIOCHEMICAL JOURNAL

The NF-κB Factor RelB and Histone H3 Lysine Methyltransferase G9a Directly Interact to Generate Epigenetic Silencing in Endotoxin Tolerance

(2009) Xiaoping Chen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Loss of the Brm-Type SWI/SNF Chromatin Remodeling Complex Is a Strong Barrier to the Tat-Independent Transcriptional Elongation of Human Immunodeficiency Virus Type 1 Transcripts

(2009) T. Mizutani et al.   JOURNAL OF VIROLOGY

Arginine Methylation Increases the Stability of Human Immunodeficiency Virus Type 1 Tat

(2009) H. Sivakumaran et al.   JOURNAL OF VIROLOGY

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

(2009) Hiba Mahdi et al.   NATURE GENETICS

Regulation of NF- B by NSD1/FBXL11-dependent reversible lysine methylation of p65

(2009) T. Lu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Systemic Inflammatory Response Syndrome (SIRS) in acutely hospitalised medical patients: a cohort study

(2009) Pål Comstedt et al.   Scandinavian Journal of Trauma Resuscitation & Emergency Medicine

Role of the Histone H3 Lysine 4 Methyltransferase, SET7/9, in the Regulation of NF-κB-dependent Inflammatory Genes

(2008) Yan Li et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A key role for autophagy and the autophagy gene Atg16l1 in mouse and human intestinal Paneth cells

(2008) Ken Cadwell et al.   NATURE

From endoplasmic-reticulum stress to the inflammatory response

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