Bromodomains as therapeutic targets

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

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

Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains

(2011) Chun-wa Chung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Ablation of CBP in Forebrain Principal Neurons Causes Modest Memory and Transcriptional Defects and a Dramatic Reduction of Histone Acetylation But Does Not Affect Cell Viability

(2011) L. M. Valor et al.   JOURNAL OF NEUROSCIENCE

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

Inactivating mutations of acetyltransferase genes in B-cell lymphoma

(2011) Laura Pasqualucci et al.   NATURE

The role of CREB signaling in Alzheimer’s disease and other cognitive disorders

(2011) Carlos A. Saura et al.   REVIEWS IN THE NEUROSCIENCES

Interaction of Propionylated and Butyrylated Histone H3 Lysine Marks with Brd4 Bromodomains

(2010) Friederike Vollmuth et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Chromatin-Remodeling Components of the BAF Complex Facilitate Reprogramming

(2010) Nishant Singhal et al.   CELL

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

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

Autoantibodies to GW bodies and other autoantigens in primary biliary cirrhosis

(2010) L. M. Stinton et al.   CLINICAL AND EXPERIMENTAL IMMUNOLOGY

ATAD2B is a phylogenetically conserved nuclear protein expressed during neuronal differentiation and tumorigenesis

(2010) Nathaniel T. Leachman et al.   DEVELOPMENT GROWTH & DIFFERENTIATION

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

(2010) Nicolas Reynoird et al.   EMBO JOURNAL

BRG1 helps RNA polymerase II to overcome a nucleosomal barrier during elongation, in vivo

(2010) Alicia Subtil-Rodríguez et al.   EMBO REPORTS

Inside HDAC with HDAC inhibitors

(2010) Philippe Bertrand   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

(2010) Shivani Malik et al.   FEBS Journal

Structural implications for K5/K12-di-acetylated histone H4 recognition by the second bromodomain of BRD2

(2010) Takashi Umehara 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

Evaluation of 172 candidate polymorphisms for association with oligozoospermia or azoospermia in a large cohort of men of European descent

(2010) K. I. Aston et al.   HUMAN REPRODUCTION

Phase I and Pharmacologic Study of SNS-032, a Potent and Selective Cdk2, 7, and 9 Inhibitor, in Patients With Advanced Chronic Lymphocytic Leukemia and Multiple Myeloma

(2010) Wei-Gang Tong et al.   JOURNAL OF CLINICAL ONCOLOGY

Chromatin Loading of E2F-MLL Complex by Cancer-Associated Coregulator ANCCA via Reading a Specific Histone Mark

(2010) A. S. Revenko et al.   MOLECULAR AND CELLULAR BIOLOGY

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

TRIM24 links a non-canonical histone signature to breast cancer

(2010) Wen-Wei Tsai et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Polybromo-associated BRG1-associated factor components BRD7 and BAF180 are critical regulators of p53 required for induction of replicative senescence

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

Transcriptional coactivators p300 and CBP stimulate estrogen receptor-beta signaling and regulate cellular events in prostate cancer

(2010) Jan Bouchal et al.   PROSTATE

The interaction of modified histones with the bromodomain testis-specific (BRDT) gene and its mRNA level in sperm of fertile donors and subfertile men

(2010) Cornelia Steilmann et al.   REPRODUCTION

Regulation of intermediary metabolism by protein acetylation

(2010) Kun-Liang Guan et al.   TRENDS IN BIOCHEMICAL SCIENCES

Brd2disruption in mice causes severe obesity without Type 2 diabetes

(2009) Fangnian Wang et al.   BIOCHEMICAL JOURNAL

The chromatin-targeting protein Brd2 is required for neural tube closure and embryogenesis

(2009) Aron Gyuris et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

TRIM24 mediates ligand-dependent activation of androgen receptor and is repressed by a bromodomain-containing protein, BRD7, in prostate cancer cells

(2009) Misato Kikuchi et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Further immunohistochemical characterization of BRD1 a new susceptibility gene for schizophrenia and bipolar affective disorder

(2009) Carsten Reidies Bjarkam et al.   Brain Structure & Function

Pharmacology of epigenetics in brain disorders

(2009) Pritika Narayan et al.   BRITISH JOURNAL OF PHARMACOLOGY

ATAD2 Is a Novel Cofactor for MYC, Overexpressed and Amplified in Aggressive Tumors

(2009) M. Ciro et al.   CANCER RESEARCH

Understanding the Words of Chromatin Regulation

(2009) Jiang I. Wu et al.   CELL

Current Perspectives on Role of Chromatin Modifications and Deacetylases in Lung Inflammation in COPD

(2009) Saravanan Rajendrasozhan et al.   COPD-Journal of Chronic Obstructive Pulmonary Disease

Double bromodomain-containing gene Brd2 is essential for embryonic development in mouse

(2009) Enyuan Shang et al.   DEVELOPMENTAL DYNAMICS

WHAT do viruses BET on?

(2009) Magdalena Weidner-Glunde   Frontiers in Bioscience-Landmark

Involvement of SMARCA2/BRM in the SWI/SNF chromatin-remodeling complex in schizophrenia

(2009) Minori Koga et al.   HUMAN MOLECULAR GENETICS

Structures of the Dual Bromodomains of the P-TEFb-activating Protein Brd4 at Atomic Resolution

(2009) Friederike Vollmuth et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Variations in the composition of mammalian SWI/SNF chromatin remodelling complexes

(2009) Jessica Ryme et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

Gallic Acid Suppresses Lipopolysaccharide-Induced Nuclear Factor- B Signaling by Preventing RelA Acetylation in A549 Lung Cancer Cells

(2009) K.-C. Choi et al.   MOLECULAR CANCER RESEARCH

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

(2009) Sarah J. Cullen et al.   MOLECULAR IMMUNOLOGY

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

(2009) Jeanne Morinière et al.   NATURE

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

(2009) Hiba Mahdi et al.   NATURE GENETICS

Syndromic features and mild cognitive impairment in mice with genetic reduction on p300 activity: Differential contribution of p300 and CBP to Rubinstein–Taybi syndrome etiology

(2009) Jose Viosca et al.   NEUROBIOLOGY OF DISEASE

An embryonic stem cell chromatin remodeling complex, esBAF, is an essential component of the core pluripotency transcriptional network

(2009) L. Ho et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2009) C. Choudhary et al.   SCIENCE

Structural Basis and Binding Properties of the Second Bromodomain of Brd4 with Acetylated Histone Tails†‡

(2008) Ying Liu et al.   BIOCHEMISTRY

Kinetic analysis of acetylation-dependent Pb1 bromodomain–histone interactions

(2008) Christopher Kupitz et al.   BIOPHYSICAL CHEMISTRY

The multi-tasking P-TEFb complex

(2008) Vanessa Brès et al.   CURRENT OPINION IN CELL BIOLOGY

The dual bromodomain and WD repeat-containing mouse protein BRWD1 is required for normal spermiogenesis and the oocyte–embryo transition

(2008) Dana L. Philipps et al.   DEVELOPMENTAL BIOLOGY

Coronary development is regulated by ATP-dependent SWI/SNF chromatin remodeling component BAF180

(2008) Xuling Huang et al.   DEVELOPMENTAL BIOLOGY

Generation of mice with a conditional allele forTrim33

(2008) Jieun Kim et al.   GENESIS

The EBNA1 Protein of Epstein-Barr Virus Functionally Interacts with Brd4

(2008) A. Lin et al.   JOURNAL OF VIROLOGY

The Double Bromodomain Proteins Brd2 and Brd3 Couple Histone Acetylation to Transcription

(2008) Gary LeRoy et al.   MOLECULAR CELL

Structural insights into human KAP1 PHD finger–bromodomain and its role in gene silencing

(2008) Lei Zeng et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Putting a KAP on Transcription and Stress

(2008) Mark D. Alter et al.   NEURON

KAP1-Mediated Epigenetic Repression in the Forebrain Modulates Behavioral Vulnerability to Stress

(2008) Johan Jakobsson et al.   NEURON

A functional genome-wide RNAi screen identifies TAF1 as a regulator for apoptosis in response to genotoxic stress

(2008) J. Kimura et al.   NUCLEIC ACIDS RESEARCH

Bromodomain 4 activation predicts breast cancer survival

(2008) N. P. S. Crawford et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Basis of Site-Specific Histone Recognition by the Bromodomains of Human Coactivators PCAF and CBP/p300

(2008) Lei Zeng et al.   STRUCTURE