Epigenetic protein families: a new frontier for drug discovery

Histone deacetylase inhibitors suppress rheumatoid arthritis fibroblast-like synoviocyte and macrophage IL-6 production by accelerating mRNA decay

(2011) Aleksander M Grabiec et al.   ANNALS OF THE RHEUMATIC DISEASES

Structural basis for CARM1 inhibition by indole and pyrazole inhibitors

(2011) John S. Sack et al.   BIOCHEMICAL JOURNAL

PR-domain-containing Mds1-Evi1 is critical for long-term hematopoietic stem cell function

(2011) Y. Zhang et al.   BLOOD

Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor

(2011) Scott R. Daigle et al.   CANCER CELL

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Class IIa Histone Deacetylases Are Hormone-Activated Regulators of FOXO and Mammalian Glucose Homeostasis

(2011) Maria M. Mihaylova et al.   CELL

Fine Tuning Our Cellular Factories: Sirtuins in Mitochondrial Biology

(2011) Lei Zhong et al.   Cell Metabolism

Regulation of chromatin by histone modifications

(2011) Andrew J Bannister et al.   CELL RESEARCH

Chemogenetic Analysis of Human Protein Methyltransferases

(2011) Victoria M. Richon et al.   Chemical Biology & Drug Design

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

(2011) Jagat C. Borah et al.   CHEMISTRY & BIOLOGY

Inhibition of Histone Demethylases by 4-Carboxy-2,2′-Bipyridyl Compounds

(2011) Kai-Hsuan Chang et al.   ChemMedChem

Histone/protein deacetylases control Foxp3 expression and the heat shock response of T-regulatory cells

(2011) Ulf H Beier et al.   CURRENT OPINION IN IMMUNOLOGY

Histone acetyltransferases are crucial regulators in NF-κB mediated inflammation

(2011) Massimo Ghizzoni et al.   DRUG DISCOVERY TODAY

The epigenetic basis of the Warburg effect

(2011) Xian Wang et al.   Epigenetics

Romidepsin: a novel histone deacetylase inhibitor for cancer

(2011) Erin M Bertino et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Structural Chemistry of the Histone Methyltransferases Cofactor Binding Site

(2011) Valérie Campagna-Slater et al.   Journal of Chemical Information and Modeling

Discovery of (2E)-3-{2-Butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an Orally Active Histone Deacetylase Inhibitor with a Superior Preclinical Profile

(2011) Haishan Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small-Molecule Ligands of Methyl-Lysine Binding Proteins

(2011) J. Martin Herold 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 2: Optimization of Phenylisoxazole Sulfonamides

(2011) Paul Bamborough et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Selective Inhibitor and Probe of the Cellular Functions of Jumonji C Domain-Containing Histone Demethylases

(2011) Xuelai Luo et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Mocetinostat for relapsed classical Hodgkin's lymphoma: an open-label, single-arm, phase 2 trial

(2011) Anas Younes et al.   LANCET ONCOLOGY

Histone Deacetylase 6 and Heat Shock Protein 90 Control the Functions of Foxp3+ T-Regulatory Cells

(2011) E. F. de Zoeten et al.   MOLECULAR AND CELLULAR BIOLOGY

Inhibition of the Acetyltransferases p300 and CBP Reveals a Targetable Function for p300 in the Survival and Invasion Pathways of Prostate Cancer Cell Lines

(2011) F. R. Santer et al.   MOLECULAR CANCER THERAPEUTICS

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(2011) Antonio Furlan et al.   MOLECULAR MEDICINE

Epigenetics: Unravelling the cancer code

(2011) Vicki Brower   NATURE

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

(2011) Johannes Zuber et al.   NATURE

Mapping and analysis of chromatin state dynamics in nine human cell types

(2011) Jason Ernst et al.   NATURE

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

(2011) Mark A. Dawson et al.   NATURE

Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

(2011) Marcus Bantscheff et al.   NATURE BIOTECHNOLOGY

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

(2011) Masoud Vedadi et al.   Nature Chemical Biology

Isothiazolones; thiol-reactive inhibitors of cysteine protease cathepsin B and histone acetyltransferase PCAF

(2011) Rosalina Wisastra et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Sirt5 Is a NAD-Dependent Protein Lysine Demalonylase and Desuccinylase

(2011) J. Du et al.   SCIENCE

Structural Basis of Substrate Methylation and Inhibition of SMYD2

(2011) Andrew D. Ferguson et al.   STRUCTURE

Histone deacetylases as regulators of inflammation and immunity

(2011) Melanie R. Shakespear et al.   TRENDS IN IMMUNOLOGY

Resveratrol regulates human adipocyte number and function in a Sirt1-dependent manner

(2010) Pamela Fischer-Posovszky et al.   AMERICAN JOURNAL OF CLINICAL NUTRITION

Haploinsufficiency of HDAC4 Causes Brachydactyly Mental Retardation Syndrome, with Brachydactyly Type E, Developmental Delays, and Behavioral Problems

(2010) Stephen R. Williams et al.   AMERICAN JOURNAL OF HUMAN GENETICS

Distribution Analysis of Deacetylase SIRT1 in Rodent and Human Nervous Systems

(2010) Sherry M. Zakhary et al.   Anatomical Record-Advances in Integrative Anatomy and Evolutionary Biology

Mammalian Sirtuins: Biological Insights and Disease Relevance

(2010) Marcia C. Haigis et al.   Annual Review of Pathology-Mechanisms of Disease

Glycemic memory associated epigenetic changes

(2010) Andrew L. Siebel et al.   BIOCHEMICAL PHARMACOLOGY

Sirtuins and inflammation: Friends or foes?

(2010) Mara Gallí et al.   BIOCHEMICAL PHARMACOLOGY

Structurally Designedtrans-2-Phenylcyclopropylamine Derivatives Potently Inhibit Histone Demethylase LSD1/KDM1,,§

(2010) Shinya Mimasu et al.   BIOCHEMISTRY

Sirtuin chemical mechanisms

(2010) Anthony A. Sauve   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Synthesis and biological activity of optically active NCL-1, a lysine-specific demethylase 1 selective inhibitor

(2010) Daisuke Ogasawara et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Toward the development of potent and selective bisubstrate inhibitors of protein arginine methyltransferases

(2010) James Dowden et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

EZH2-mediated epigenetic silencing in germinal center B cells contributes to proliferation and lymphomagenesis

(2010) I. Velichutina et al.   BLOOD

Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation

(2010) D. B. Yap et al.   BLOOD

The novel inhibitor of histone deacetylase resminostat (RAS2410) inhibits proliferation and induces apoptosis in multiple myeloma (MM) cells

(2010) Sonja Mandl-Weber et al.   BRITISH JOURNAL OF HAEMATOLOGY

CUDC-101, a Multitargeted Inhibitor of Histone Deacetylase, Epidermal Growth Factor Receptor, and Human Epidermal Growth Factor Receptor 2, Exerts Potent Anticancer Activity

(2010) Cheng-Jung Lai et al.   CANCER RESEARCH

ANCCA/ATAD2 Overexpression Identifies Breast Cancer Patients with Poor Prognosis, Acting to Drive Proliferation and Survival of Triple-Negative Cells through Control of B-Myb and EZH2

(2010) E. V. Kalashnikova et al.   CANCER RESEARCH

Virtual Ligand Screening of the p300/CBP Histone Acetyltransferase: Identification of a Selective Small Molecule Inhibitor

(2010) Erin M. Bowers et al.   CHEMISTRY & BIOLOGY

CBP Histone Acetyltransferase Activity Regulates Embryonic Neural Differentiation in the Normal and Rubinstein-Taybi Syndrome Brain

(2010) Jing Wang et al.   DEVELOPMENTAL CELL

Epigenetic therapies for non-oncology indications

(2010) Jonathan D. Best et al.   DRUG DISCOVERY TODAY

The clinical development of histone deacetylase inhibitors as targeted anticancer drugs

(2010) Paul A Marks   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Histone arginine methylation

(2010) Alessandra Di Lorenzo et al.   FEBS LETTERS

SMARCA2 and other genome-wide supported schizophrenia-associated genes: regulation by REST/NRSF, network organization and primate-specific evolution

(2010) Yann Loe-Mie et al.   HUMAN MOLECULAR GENETICS

SAHA ameliorates the SMA phenotype in two mouse models for spinal muscular atrophy

(2010) Markus Riessland et al.   HUMAN MOLECULAR GENETICS

p300-mediated Acetylation of Histone H3 Lysine 56 Functions in DNA Damage Response in Mammals

(2010) Rahul K. Vempati et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

SRT1720, SRT2183, SRT1460, and Resveratrol Are Not Direct Activators of SIRT1

(2010) Michelle Pacholec et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Resveratrol Potentiates Glucose-stimulated Insulin Secretion in INS-1E β-Cells and Human Islets through a SIRT1-dependent Mechanism

(2010) Laurène Vetterli et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Epigenetic basis for aberrant upregulation of autoantigen genes in humans with ANCA vasculitis

(2010) Dominic J. Ciavatta et al.   JOURNAL OF CLINICAL INVESTIGATION

Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines.

(2010) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Adding a Lysine Mimic in the Design of Potent Inhibitors of Histone Lysine Methyltransferases

(2010) Yanqi Chang et al.   JOURNAL OF MOLECULAR BIOLOGY

Differential Histone Deacetylase mRNA Expression Patterns in Amyotrophic Lateral Sclerosis

(2010) Claas Janssen et al.   JOURNAL OF NEUROPATHOLOGY AND EXPERIMENTAL NEUROLOGY

CREB Binding Protein Is Required for Both Short-Term and Long-Term Memory Formation

(2010) G. Chen et al.   JOURNAL OF NEUROSCIENCE

Comparative Analysis of Small Molecules and Histone Substrate Analogues as LSD1 Lysine Demethylase Inhibitors

(2010) Jeffrey C. Culhane et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Biochemical, Structural, and Biological Evaluation of Tranylcypromine Derivatives as Inhibitors of Histone Demethylases LSD1 and LSD2

(2010) Claudia Binda et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

SB939, a Novel Potent and Orally Active Histone Deacetylase Inhibitor with High Tumor Exposure and Efficacy in Mouse Models of Colorectal Cancer

(2010) V. Novotny-Diermayr et al.   MOLECULAR CANCER THERAPEUTICS

A Functional Link between the Histone Demethylase PHF8 and the Transcription Factor ZNF711 in X-Linked Mental Retardation

(2010) Daniela Kleine-Kohlbrecher et al.   MOLECULAR CELL

A Feed-Forward Circuit Controlling Inducible NF-κB Target Gene Activation by Promoter Histone Demethylation

(2010) Dominic van Essen et al.   MOLECULAR CELL

Chemical biology of Histone acetyltransferase natural compounds modulators

(2010) Fabrizio Dal Piaz et al.   MOLECULAR DIVERSITY

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

The landscape of somatic copy-number alteration across human cancers

(2010) Rameen Beroukhim et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Epigenetic modifications as therapeutic targets

(2010) Theresa K Kelly et al.   NATURE BIOTECHNOLOGY

Epigenetic modifications and human disease

(2010) Anna Portela et al.   NATURE BIOTECHNOLOGY

Epigenetic modifications in pluripotent and differentiated cells

(2010) Alexander Meissner   NATURE BIOTECHNOLOGY

Chemical phylogenetics of histone deacetylases

(2010) James E Bradner et al.   Nature Chemical Biology

Epigenetic regulation of the neural transcriptome: the meaning of the marks

(2010) Michael J Meaney et al.   NATURE NEUROSCIENCE

53BP1 loss rescues BRCA1 deficiency and is associated with triple-negative and BRCA-mutated breast cancers

(2010) Peter Bouwman et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Functional characterization of ATAD2 as a new cancer/testis factor and a predictor of poor prognosis in breast and lung cancers

(2010) C Caron et al.   ONCOGENE

The Novel Deacetylase Inhibitor AR-42 Demonstrates Pre-Clinical Activity in B-Cell Malignancies In Vitro and In Vivo

(2010) David M. Lucas et al.   PLoS One

Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors

(2010) Oliver N. F. King et al.   PLoS One

The Genetic Landscape of the Childhood Cancer Medulloblastoma

(2010) D. W. Parsons et al.   SCIENCE

SIRT1 inhibits inflammatory pathways in macrophages and modulates insulin sensitivity

(2009) Takeshi Yoshizaki et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Protective Role of SIRT1 in Diabetic Vascular Dysfunction

(2009) Masayuki Orimo et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Epigenetic regulation of the alternatively activated macrophage phenotype

(2009) M. Ishii et al.   BLOOD

Small Molecules Efficiently Direct Endodermal Differentiation of Mouse and Human Embryonic Stem Cells

(2009) Malgorzata Borowiak et al.   Cell Stem Cell

The Emerging Therapeutic Potential of Histone Methyltransferase and Demethylase Inhibitors

(2009) Astrid Spannhoff et al.   ChemMedChem

Clinical Studies of Histone Deacetylase Inhibitors

(2009) H. M. Prince et al.   CLINICAL CANCER RESEARCH

TIMP3 Is Reduced in Atherosclerotic Plaques From Subjects With Type 2 Diabetes and Increased by SirT1

(2009) M. Cardellini et al.   DIABETES

SIRT1 Genetic Variation Is Related to BMI and Risk of Obesity

(2009) M.Carola Zillikens et al.   DIABETES

Hyperglycemia Induces a Dynamic Cooperativity of Histone Methylase and Demethylase Enzymes Associated With Gene-Activating Epigenetic Marks That Coexist on the Lysine Tail

(2009) D. Brasacchio et al.   DIABETES

Histone acetyl transferases as emerging drug targets

(2009) Frank J. Dekker et al.   DRUG DISCOVERY TODAY

Epigenetic opportunities and challenges in cancer

(2009) Jonathan D. Best et al.   DRUG DISCOVERY TODAY

Jmjd3 contributes to the control of gene expression in LPS-activated macrophages

(2009) Francesca De Santa et al.   EMBO JOURNAL

Central Administration of Resveratrol Improves Diet-Induced Diabetes

(2009) Giorgio Ramadori et al.   ENDOCRINOLOGY

Identification and Characterization of Propionylation at Histone H3 Lysine 23 in Mammalian Cells

(2009) Bo Liu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

Further clinical and molecular delineation of the 9q subtelomeric deletion syndrome supports a major contribution of EHMT1 haploinsufficiency to the core phenotype

(2009) T Kleefstra et al.   JOURNAL OF MEDICAL GENETICS

Novel Cambinol Analogs as Sirtuin Inhibitors: Synthesis, Biological Evaluation, and Rationalization of Activity

(2009) Federico Medda et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antidepressant Actions of Histone Deacetylase Inhibitors

(2009) H. E. Covington et al.   JOURNAL OF NEUROSCIENCE

CBP/p300-mediated acetylation of histone H3 on lysine 56

(2009) Chandrima Das et al.   NATURE

Haematopoietic malignancies caused by dysregulation of a chromatin-binding PHD finger

(2009) Gang G. Wang et al.   NATURE

Multiple recurrent genetic events converge on control of histone lysine methylation in medulloblastoma

(2009) Paul A Northcott et al.   NATURE GENETICS

Protein methyltransferases as a target class for drug discovery

(2009) Robert A. Copeland et al.   NATURE REVIEWS DRUG DISCOVERY

Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294

(2009) Yanqi Chang et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Control of Cognition and Adaptive Behavior by the GLP/G9a Epigenetic Suppressor Complex

(2009) Anne Schaefer et al.   NEURON

Lysine Acetylation Targets Protein Complexes and Co-Regulates Major Cellular Functions

(2009) C. Choudhary et al.   SCIENCE

A Combined Chemical and Genetic Approach for the Generation of Induced Pluripotent Stem Cells

(2008) Yan Shi et al.   Cell Stem Cell

Histone Deacetylase 8 in Neuroblastoma Tumorigenesis

(2008) I. Oehme et al.   CLINICAL CANCER RESEARCH

XLMR genes: update 2007

(2008) Pietro Chiurazzi et al.   EUROPEAN JOURNAL OF HUMAN GENETICS

Genetic and epigenetic defects in mental retardation

(2008) Jamie M. Kramer et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Human HDAC7 Harbors a Class IIa Histone Deacetylase-specific Zinc Binding Motif and Cryptic Deacetylase Activity

(2008) Anja Schuetz et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases⊥

(2008) Nathan R. Rose et al.   JOURNAL OF MEDICINAL CHEMISTRY

Transgenerational effects of prenatal nutrient restriction on cardiovascular and hypothalamic-pituitary-adrenal function

(2008) Caroline Bertram et al.   JOURNAL OF PHYSIOLOGY-LONDON

MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo

(2008) M. Fournel et al.   MOLECULAR CANCER THERAPEUTICS

Roles of the EZH2 histone methyltransferase in cancer epigenetics

(2008) Jeffrey A. Simon et al.   MUTATION RESEARCH-FUNDAMENTAL AND MOLECULAR MECHANISMS OF MUTAGENESIS

The structural basis of protein acetylation by the p300/CBP transcriptional coactivator

(2008) Xin Liu et al.   NATURE

SIRT6 is a histone H3 lysine 9 deacetylase that modulates telomeric chromatin

(2008) Eriko Michishita et al.   NATURE

Induction of pluripotent stem cells from primary human fibroblasts with only Oct4 and Sox2

(2008) Danwei Huangfu et al.   NATURE BIOTECHNOLOGY