Targeting Cancer Cells with BET Bromodomain Inhibitors

RVX-297- a novel BD2 selective inhibitor of BET bromodomains

(2016) Olesya A. Kharenko et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Preclinical Anticancer Efficacy of BET Bromodomain Inhibitors Is Determined by the Apoptotic Response

(2016) Andrew R. Conery et al.   CANCER RESEARCH

Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer

(2016) Shaokun Shu et al.   NATURE

BRD4 is a histone acetyltransferase that evicts nucleosomes from chromatin

(2016) Ballachanda N Devaiah et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structure of the Brd4 ET domain bound to a C-terminal motif from γ-retroviral integrases reveals a conserved mechanism of interaction

(2016) Brandon L. Crowe et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Mechanism of Transcriptional Regulator NSD3 Recognition by the ET Domain of BRD4

(2016) Qiang Zhang et al.   STRUCTURE

Clinical Response of Carcinomas Harboring the BRD4-NUT Oncoprotein to the Targeted Bromodomain Inhibitor OTX015/MK-8628

(2016) A. Stathis et al.   Cancer Discovery

BRD4 Connects Enhancer Remodeling to Senescence Immune Surveillance

(2016) N. Tasdemir et al.   Cancer Discovery

BRD4 is a histone acetyltransferase that evicts nucleosomes from chromatin

(2016) Ballachanda N Devaiah et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Targeting BET bromodomain proteins in solid tumors

(2016) Vaibhav Sahai et al.   Oncotarget

BET Bromodomain Inhibition Releases the Mediator Complex from Select cis -Regulatory Elements

(2016) Anand S. Bhagwat et al.   Cell Reports

Bromodomain inhibitor OTX015 in patients with acute leukaemia: a dose-escalation, phase 1 study

(2016) Céline Berthon et al.   Lancet Haematology

Bromodomain inhibitor OTX015 in patients with lymphoma or multiple myeloma: a dose-escalation, open-label, pharmacokinetic, phase 1 study

(2016) Sandy Amorim et al.   Lancet Haematology

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

(2015) Michael Zengerle et al.   ACS Chemical Biology

Functions of BET proteins in erythroid gene expression

(2015) Aaron J. Stonestrom et al.   BLOOD

Kinase and BET Inhibitors Together Clamp Inhibition of PI3K Signaling and Overcome Resistance to Therapy

(2015) Elias E. Stratikopoulos et al.   CANCER CELL

BRAD4 plays a critical role in germinal center response by regulating Bcl-6 and NF-κB activation

(2015) Fangjie Gao et al.   CELLULAR IMMUNOLOGY

Protein Lysine Acetylation by p300/CBP

(2015) Beverley M. Dancy et al.   CHEMICAL REVIEWS

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition

(2015) A. Henssen et al.   CLINICAL CANCER RESEARCH

The oncogenic BRD4-NUT chromatin regulator drives aberrant transcription within large topological domains

(2015) Artyom A. Alekseyenko et al.   GENES & DEVELOPMENT

Autism-like syndrome is induced by pharmacological suppression of BET proteins in young mice

(2015) Josefa M. Sullivan et al.   JOURNAL OF EXPERIMENTAL MEDICINE

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

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

BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia

(2015) Jae-Seok Roe et al.   MOLECULAR CELL

NSD3-Short Is an Adaptor Protein that Couples BRD4 to the CHD8 Chromatin Remodeler

(2015) Chen Shen et al.   MOLECULAR CELL

Transcriptional plasticity promotes primary and acquired resistance to BET inhibition

(2015) Philipp Rathert et al.   NATURE

BET inhibitor resistance emerges from leukaemia stem cells

(2015) Chun Yew Fong et al.   NATURE

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

(2015) Erica Korb et al.   NATURE NEUROSCIENCE

The Mediator complex: a central integrator of transcription

(2015) Benjamin L. Allen et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Getting up to speed with transcription elongation by RNA polymerase II

(2015) Iris Jonkers et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

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

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

Disrupting the Interaction of BRD4 with Diacetylated Twist Suppresses Tumorigenesis in Basal-like Breast Cancer

(2014) Jian Shi et al.   CANCER CELL

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

Mechanistic Analysis of the Role of Bromodomain-containing Protein 4 (BRD4) in BRD4-NUT Oncoprotein-induced Transcriptional Activation

(2014) Ranran Wang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

An epigenetic mechanism of resistance to targeted therapy in T cell acute lymphoblastic leukemia

(2014) Birgit Knoechel et al.   NATURE GENETICS

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

NSD3-NUT Fusion Oncoprotein in NUT Midline Carcinoma: Implications for a Novel Oncogenic Mechanism

(2014) C. A. French et al.   Cancer Discovery

Inducible In Vivo Silencing of Brd4 Identifies Potential Toxicities of Sustained BET Protein Inhibition

(2014) Jessica E. Bolden et al.   Cell Reports

Bromodomain Protein BRD4 Is Required for Estrogen Receptor-Dependent Enhancer Activation and Gene Transcription

(2014) Sankari Nagarajan et al.   Cell Reports

Transformation Resistance in a Premature Aging Disorder Identifies a Tumor-Protective Function of BRD4

(2014) Patricia Fernandez et al.   Cell Reports

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

Discovery and Characterization of Super-Enhancer-Associated Dependencies in Diffuse Large B Cell Lymphoma

(2013) Bjoern Chapuy et al.   CANCER CELL

A multi-histology trial of fostamatinib in patients with advanced colorectal, non-small cell lung, head and neck, thyroid, and renal cell carcinomas, and pheochromocytomas

(2013) Sook Ryun Park et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

Master Transcription Factors and Mediator Establish Super-Enhancers at Key Cell Identity Genes

(2013) Warren A. Whyte et al.   CELL

Super-Enhancers in the Control of Cell Identity and Disease

(2013) Denes Hnisz et al.   CELL

Brd4 and JMJD6-Associated Anti-Pause Enhancers in Regulation of Transcriptional Pause Release

(2013) Wen Liu et al.   CELL

BET Bromodomains Mediate Transcriptional Pause Release in Heart Failure

(2013) Priti Anand et al.   CELL

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

(2013) Guangtao Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Chromatin stretch enhancer states drive cell-specific gene regulation and harbor human disease risk variants

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

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

A Structural Basis for BRD2/4-Mediated Host Chromatin Interaction and Oligomer Assembly of Kaposi Sarcoma-Associated Herpesvirus and Murine Gammaherpesvirus LANA Proteins

(2013) Jan Hellert et al.   PLoS Pathogens

ApoA-I Induction as a Potential Cardioprotective Strategy: Rationale for the SUSTAIN and ASSURE Studies

(2012) Stephen J. Nicholls et al.   CARDIOVASCULAR DRUGS AND THERAPY

Small-Molecule Inhibition of BRDT for Male Contraception

(2012) Martin M. Matzuk et al.   CELL

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

(2012) Panagis Filippakopoulos et al.   CELL

Down-regulation of NF-κB Transcriptional Activity in HIV-associated Kidney Disease by BRD4 Inhibition

(2012) Guangtao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

Suppression of the antiviral response by an influenza histone mimic

(2012) Ivan Marazzi et al.   NATURE

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

(2012) Zichong Li et al.   NUCLEIC ACIDS RESEARCH

BRD4 is an atypical kinase that phosphorylates Serine2 of the RNA Polymerase II carboxy-terminal domain

(2012) B. N. Devaiah et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Reactivation of Latent HIV-1 by Inhibition of BRD4

(2012) Jian Zhu et al.   Cell Reports

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

(2011) Jake E. Delmore et al.   CELL

Perturbation of BRD4 Protein Function by BRD4-NUT Protein Abrogates Cellular Differentiation in NUT Midline Carcinoma

(2011) Junpeng Yan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Efficacy and Safety of a Novel Oral Inducer of Apolipoprotein A-I Synthesis in Statin-Treated Patients With Stable Coronary Artery Disease

(2011) Stephen J. Nicholls et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

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

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

NUT midline carcinoma

(2010) Christopher Alexander French   CANCER GENETICS AND CYTOGENETICS

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

(2010) Nicolas Reynoird et al.   EMBO JOURNAL

RVX-208

(2010) Dana Bailey et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

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

CDK8 is a positive regulator of transcriptional elongation within the serum response network

(2010) Aaron J Donner et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The Mechanism of Release of P-TEFb and HEXIM1 from the 7SK snRNP by Viral and Cellular Activators Includes a Conformational Change in 7SK

(2010) Brian J. Krueger et al.   PLoS One

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

(2009) Jeanne Morinière et al.   NATURE

Combinatorial patterns of histone acetylations and methylations in the human genome

(2008) Zhibin Wang et al.   NATURE GENETICS