The Functions of BET Proteins in Gene Transcription of Biology and Diseases

Acute perturbation strategies in interrogating RNA polymerase II elongation factor function in gene expression

(2021) Bin Zheng et al.   GENES & DEVELOPMENT

BET inhibition disrupts transcription but retains enhancer-promoter contact

(2021) Nicholas T. Crump et al.   Nature Communications

BET-Family Bromodomains Can Recognize Diacetylated Sequences from Transcription Factors Using a Conserved Mechanism

(2021) Karishma Patel et al.   BIOCHEMISTRY

Long Noncoding RNA NEAT1 Acts as a Molecular Switch for BRD4 Transcriptional Activity and Mediates Repression of BRD4/WDR5 Target Genes

(2021) Mariaelena Pistoni et al.   MOLECULAR CANCER RESEARCH

Co-condensation between transcription factor and coactivator p300 modulates transcriptional bursting kinetics

(2021) Liang Ma et al.   MOLECULAR CELL

Reentrant liquid condensate phase of proteins is stabilized by hydrophobic and non-ionic interactions

(2021) Georg Krainer et al.   Nature Communications

Bromodomain protein BRDT directs ΔNp63 function and super-enhancer activity in a subset of esophageal squamous cell carcinomas

(2021) Xin Wang et al.   CELL DEATH AND DIFFERENTIATION

BRD4S Interacts with Viral E2 Protein To Limit Human Papillomavirus Late Transcription

(2021) A. Yigitliler et al.   JOURNAL OF VIROLOGY

PCAF ‐mediated acetylation of ISX recruits BRD 4 to promote epithelial‐mesenchymal transition

(2020) Li‐Ting Wang et al.   EMBO REPORTS

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

(2020) Emily J. Faivre et al.   NATURE

JMJD6 cleaves MePCE to release positive transcription elongation factor b (P-TEFb) in higher eukaryotes

(2020) Schuyler Lee et al.   eLife

Differential activation of P-TEFb complexes in the development of cardiomyocyte hypertrophy following activation of distinct GPCRs

(2020) Ryan D. Martin et al.   MOLECULAR AND CELLULAR BIOLOGY

Opposing Functions of BRD4 Isoforms in Breast Cancer

(2020) Shwu-Yuan Wu et al.   MOLECULAR CELL

Phase separation of TAZ compartmentalizes the transcription machinery to promote gene expression

(2020) Yi Lu et al.   NATURE CELL BIOLOGY

Roles of the BRD4 short isoform in phase separation and active gene transcription

(2020) Xinye Han et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

MYC protein stability is negatively regulated by BRD4

(2020) Ballachanda N. Devaiah et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation

(2020) Omer Gilan et al.   SCIENCE

p300-Mediated Acetylation of Histone Demethylase JMJD1A Prevents Its Degradation by Ubiquitin Ligase STUB1 and Enhances Its Activity in Prostate Cancer

(2020) Songhui Xu et al.   CANCER RESEARCH

PHF7 Modulates BRDT Stability and Histone-to-Protamine Exchange during Spermiogenesis

(2020) Chang Rok Kim et al.   Cell Reports

ASXL3 bridges BRD4 to BAP1 complex and governs enhancer activity in small cell lung cancer

(2020) Aileen Patricia Szczepanski et al.   Genome Medicine

lncRNA DIGIT and BRD3 protein form phase-separated condensates to regulate endoderm differentiation

(2020) Kaveh Daneshvar et al.   NATURE CELL BIOLOGY

BRDT is a novel regulator of eIF4EBP1 in renal cell carcinoma

(2020) Pei Wan et al.   ONCOLOGY REPORTS

BRD4 prevents the accumulation of R-loops and protects against transcription–replication collision events and DNA damage

(2020) Fred C. Lam et al.   Nature Communications

BRD4 Prevents R-Loop Formation and Transcription-Replication Conflicts by Ensuring Efficient Transcription Elongation

(2020) Drake S. Edwards et al.   Cell Reports

Integration of the Transcriptome and Genome-Wide Landscape of BRD2 and BRD4 Binding Motifs Identifies Key Superenhancer Genes and Reveals the Mechanism of Bet Inhibitor Action in Rheumatoid Arthritis Synovial Fibroblasts

(2020) Vinod Krishna et al.   JOURNAL OF IMMUNOLOGY

The bromodomains of BET family proteins can recognize diacetylated histone H2A .Z

(2020) Karishma Patel et al.   PROTEIN SCIENCE

circNR3C1 Suppresses Bladder Cancer Progression through Acting as an Endogenous Blocker of BRD4/C-myc Complex

(2020) Fei Xie et al.   Molecular Therapy-Nucleic Acids

Decreased miR-29b expression is associated with airway inflammation in chronic obstructive pulmonary disease

(2019) Kun Tang et al.   AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY

Long non-coding RNA LINC00346 promotes pancreatic cancer growth and gemcitabine resistance by sponging miR-188-3p to derepress BRD4 expression

(2019) Weidong Shi et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

BRD4 directs hematopoietic stem cell development and modulates macrophage inflammatory responses

(2019) Anup Dey et al.   EMBO JOURNAL

Role of BRD4 phosphorylation in the nucleus accumbens in relapse to cocaine‐seeking behavior in mice

(2019) Wei Guo et al.   ADDICTION BIOLOGY

BRD4 promotes gastric cancer progression and metastasis through acetylation-dependent stabilization of Snail

(2019) Zhong-yi Qin et al.   CANCER RESEARCH

Targeted and Interactome Proteomics Revealed the Role of PHD2 in Regulating BRD4 Proline Hydroxylation

(2019) Luke N Erber et al.   MOLECULAR & CELLULAR PROTEOMICS

JMJD6 is a tumorigenic factor and therapeutic target in neuroblastoma

(2019) Matthew Wong et al.   Nature Communications

Distinct Roles for BET Family Members in Estrogen Receptor α Enhancer Function and Gene Regulation in Breast Cancer Cells

(2019) Shino Murakami et al.   MOLECULAR CANCER RESEARCH

Organization of Chromatin by Intrinsic and Regulated Phase Separation

(2019) Bryan A. Gibson et al.   CELL

Systematic bromodomain protein screens identify homologous recombination and R-loop suppression pathways involved in genome integrity

(2019) Jae Jin Kim et al.   GENES & DEVELOPMENT

Bromodomain biology and drug discovery

(2019) Nilesh Zaware et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The Bromodomain Protein 4 Contributes to the Regulation of Alternative Splicing

(2019) Sheetal Uppal et al.   Cell Reports

Comparative structure-function analysis of bromodomain and extraterminal motif (BET) proteins in a gene-complementation system

(2019) Michael T. Werner et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting Bromodomain and Extra-Terminal (BET) Family Proteins in Castration-Resistant Prostate Cancer (CRPC)

(2018) Jonathan Welti et al.   CLINICAL CANCER RESEARCH

A mechanism for epigenetic control of DNA replication

(2018) Courtney G. Sansam et al.   GENES & DEVELOPMENT

The BRD3 ET domain recognizes a short peptide motif through a mechanism that is conserved across chromatin remodelers and transcriptional regulators

(2018) Dorothy C. C. Wai et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

BET Proteins Exhibit Transcriptional and Functional Opposition in the Epithelial-to-Mesenchymal Transition

(2018) Guillaume P. Andrieu et al.   MOLECULAR CANCER RESEARCH

OUP accepted manuscript

(2018)   NUCLEIC ACIDS RESEARCH

BRD4 facilitates replication stress-induced DNA damage response

(2018) Jingwen Zhang et al.   ONCOGENE

Coactivator condensation at super-enhancers links phase separation and gene control

(2018) Benjamin R. Sabari et al.   SCIENCE

Publisher Correction: miR-3140 suppresses tumor cell growth by targeting BRD4 via its coding sequence and downregulates the BRD4-NUT fusion oncoprotein

(2018) Erina Tonouchi et al.   Scientific Reports

BRD4 Promotes DNA Repair and Mediates the Formation of TMPRSS2-ERG Gene Rearrangements in Prostate Cancer

(2018) Xiangyi Li et al.   Cell Reports

DUB3 Promotes BET Inhibitor Resistance and Cancer Progression by Deubiquitinating BRD4

(2018) Xin Jin et al.   MOLECULAR CELL

mRNA circularization by METTL3–eIF3h enhances translation and promotes oncogenesis

(2018) Junho Choe et al.   NATURE

RNAs interact with BRD4 to promote enhanced chromatin engagement and transcription activation

(2018) Homa Rahnamoun et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Polycomb complexes associate with enhancers and promote oncogenic transcriptional programs in cancer through multiple mechanisms

(2018) Ho Lam Chan et al.   Nature Communications

Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains

(2018) Jean-Philippe Lambert et al.   MOLECULAR CELL

A non-canonical BRD9-containing BAF chromatin remodeling complex regulates naive pluripotency in mouse embryonic stem cells

(2018) Jovylyn Gatchalian et al.   Nature Communications

SRPK1 maintains acute myeloid leukemia through effects on isoform usage of epigenetic regulators including BRD4

(2018) Konstantinos Tzelepis et al.   Nature Communications

BET Inhibition Induces HEXIM1- and RAD51-Dependent Conflicts between Transcription and Replication

(2018) Akhil Bowry et al.   Cell Reports

Brd4’s Bromodomains Mediate Histone H3 Acetylation and Chromatin Remodeling in Pluripotent Cells through P300 and Brg1

(2018) Tao Wu et al.   Cell Reports

Bivalent complexes of PRC1 with orthologs of BRD4 and MOZ/MORF target developmental genes inDrosophila

(2017) Hyuckjoon Kang et al.   GENES & DEVELOPMENT

Altered hydroxymethylation is seen at regulatory regions in pancreatic cancer and regulates oncogenic pathways

(2017) Sanchari Bhattacharyya et al.   GENOME RESEARCH

The Short Isoform of BRD4 Promotes HIV-1 Latency by Engaging Repressive SWI/SNF Chromatin-Remodeling Complexes

(2017) Ryan J. Conrad et al.   MOLECULAR CELL

Harnessing BET Inhibitor Sensitivity Reveals AMIGO2 as a Melanoma Survival Gene

(2017) Barbara Fontanals-Cirera et al.   MOLECULAR CELL

Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and Lysosomal Function

(2017) Jun-ichi Sakamaki et al.   MOLECULAR CELL

The BET Protein BRD2 Cooperates with CTCF to Enforce Transcriptional and Architectural Boundaries

(2017) Sarah C. Hsu et al.   MOLECULAR CELL

Distinct Roles of Brd2 and Brd4 in Potentiating the Transcriptional Program for Th17 Cell Differentiation

(2017) Ka Lung Cheung et al.   MOLECULAR CELL

Prostate cancer–associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4

(2017) Xiangpeng Dai et al.   NATURE MEDICINE

Intrinsic BET inhibitor resistance in SPOP-mutated prostate cancer is mediated by BET protein stabilization and AKT–mTORC1 activation

(2017) Pingzhao Zhang et al.   NATURE MEDICINE

Opposing effects of cancer-type-specific SPOP mutants on BET protein degradation and sensitivity to BET inhibitors

(2017) Hana Janouskova et al.   NATURE MEDICINE

Prolyl isomerase PIN1 regulates the stability, transcriptional activity and oncogenic potential of BRD4

(2017) X Hu et al.   ONCOGENE

BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice

(2017) Kalung Cheung et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Uncovering BRD4 hyperphosphorylation associated with cellular transformation in NUT midline carcinoma

(2017) Ranran Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Mechanism of the Oxygenase JMJD6 Recognition by the Extraterminal (ET) Domain of BRD4

(2017) Tsuyoshi Konuma et al.   Scientific Reports

BRD3 and BRD4 BET Bromodomain Proteins Differentially Regulate Skeletal Myogenesis

(2017) Thomas C. Roberts et al.   Scientific Reports

Spatially restricted loading of BRD2 at DNA double-strand breaks protects H4 acetylation domains and promotes DNA repair

(2017) Ozge Gursoy-Yuzugullu et al.   Scientific Reports

Bromodomain Inhibitors Correct Bioenergetic Deficiency Caused by Mitochondrial Disease Complex I Mutations

(2016) Joeva J. Barrow et al.   MOLECULAR CELL

Dynamic Competing Histone H4 K5K8 Acetylation and Butyrylation Are Hallmarks of Highly Active Gene Promoters

(2016) Afsaneh Goudarzi et al.   MOLECULAR CELL

Molecular Coupling of Histone Crotonylation and Active Transcription by AF9 YEATS Domain

(2016) Yuanyuan Li et al.   MOLECULAR CELL

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

The bromodomain protein BRD4 regulates splicing during heat shock

(2016) Michelle Hussong et al.   NUCLEIC ACIDS RESEARCH

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

(2016) Qiang Zhang et al.   STRUCTURE

A bromodomain–DNA interaction facilitates acetylation-dependent bivalent nucleosome recognition by the BET protein BRDT

(2016) Thomas C. R. Miller et al.   Nature Communications

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

Signal-Dependent Recruitment of BRD4 to Cardiomyocyte Super-Enhancers Is Suppressed by a MicroRNA

(2016) Matthew S. Stratton et al.   Cell Reports

Reading and Interpreting the Histone Acylation Code

(2016) Jelly H.M. Soffers et al.   GENOMICS PROTEOMICS & BIOINFORMATICS

BET Protein BRDT Complexes With HDAC1, PRMT5, and TRIM28 and Functions in Transcriptional Repression During Spermatogenesis

(2015) Li Wang et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

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

Histone Variant H2A.Z.2 Mediates Proliferation and Drug Sensitivity of Malignant Melanoma

(2015) Chiara Vardabasso et al.   MOLECULAR CELL

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

(2015) Erica Korb et al.   NATURE NEUROSCIENCE

Getting up to speed with transcription elongation by RNA polymerase II

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

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

(2015) E. Megan Flynn et al.   STRUCTURE

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

(2014) Jian Shi et al.   CANCER CELL

Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer

(2014) Irfan A. Asangani et al.   NATURE

BRD4 assists elongation of both coding and enhancer RNAs by interacting with acetylated histones

(2014) Tomohiko Kanno et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

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

Control of Embryonic Stem Cell Identity by BRD4-Dependent Transcriptional Elongation of Super-Enhancer-Associated Pluripotency Genes

(2014) Raffaella Di Micco et al.   Cell Reports

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

BET Bromodomains Mediate Transcriptional Pause Release in Heart Failure

(2013) Priti Anand et al.   CELL

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

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

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

(2012) Panagis Filippakopoulos et al.   CELL

Insights into Role of Bromodomain, Testis-specific (Brdt) in Acetylated Histone H4-dependent Chromatin Remodeling in Mammalian Spermiogenesis

(2012) Surbhi Dhar 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

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

(2011) Jake E. Delmore et al.   CELL

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

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

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

Brd2disruption in mice causes severe obesity without Type 2 diabetes

(2009) Fangnian Wang et al.   BIOCHEMICAL JOURNAL

Control of Inducible Gene Expression by Signal-Dependent Transcriptional Elongation

(2009) Diana C. Hargreaves et al.   CELL

Histone Crosstalk between H3S10ph and H4K16ac Generates a Histone Code that Mediates Transcription Elongation

(2009) Alessio Zippo et al.   CELL

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

(2009) Enyuan Shang et al.   DEVELOPMENTAL DYNAMICS

Brd4 Regulation of Papillomavirus Protein E2 Stability

(2009) G. Zheng et al.   JOURNAL OF VIROLOGY

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

(2009) Jeanne Morinière et al.   NATURE

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

(2008) Gary LeRoy et al.   MOLECULAR CELL