Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development
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Title
Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development
Authors
Keywords
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Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 64, Issue 5, Pages 2419-2435
Publisher
American Chemical Society (ACS)
Online
2021-02-23
DOI
10.1021/acs.jmedchem.0c01487
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Note: Only part of the references are listed.- Potent Dual BET/HDAC Inhibitors for Efficient Treatment of Pancreatic Cancer
- (2020) Shipeng He et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Dual-target kinase drug design: Current strategies and future directions in cancer therapy
- (2020) Dejuan Sun et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer
- (2020) Emily J. Faivre et al. NATURE
- Make your best BET: The emerging role of BET inhibitor treatment in malignant tumors
- (2020) Oliver Bechter et al. PHARMACOLOGY & THERAPEUTICS
- Antibody–PROTAC Conjugates Enable HER2-Dependent Targeted Protein Degradation of BRD4
- (2020) Marı́a Maneiro et al. ACS Chemical Biology
- Discovery of Thieno[2,3-d]pyrimidine-Based Hydroxamic Acid Derivatives as Bromodomain-Containing Protein 4/Histone Deacetylase Dual Inhibitors Induce Autophagic Cell Death in Colorectal Carcinoma Cells
- (2020) Zhaoping Pan et al. JOURNAL OF MEDICINAL CHEMISTRY
- Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy
- (2020) Tingting Liu et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain
- (2020) George S. Sheppard et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation
- (2020) Zhiqing Liu et al. JOURNAL OF MEDICINAL CHEMISTRY
- Novel dual BET and PLK1 inhibitor WNY0824 exerts potent anti-tumor effects in CRPC by inhibiting transcription factor function and inducing mitotic abnormality
- (2020) Ying Xu et al. MOLECULAR CANCER THERAPEUTICS
- Chromatin Hyperacetylation Impacts Chromosome Folding by Forming a Nuclear Subcompartment
- (2020) Celeste D. Rosencrance et al. MOLECULAR CELL
- Opposing Functions of BRD4 Isoforms in Breast Cancer
- (2020) Shwu-Yuan Wu et al. MOLECULAR CELL
- Synthetic Lethal and Resistance Interactions with BET Bromodomain Inhibitors in Triple-Negative Breast Cancer
- (2020) Shaokun Shu et al. MOLECULAR CELL
- Targeting Hippo coactivator YAP1 through BET bromodomain inhibition in esophageal adenocarcinoma
- (2020) Shumei Song et al. Molecular Oncology
- 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
- Acquired resistance to combined BET and CDK4/6 inhibition in triple-negative breast cancer
- (2020) Jennifer Y. Ge et al. Nature Communications
- Bromodomain-selective BET inhibitors are potent antitumor agents against MYC-driven pediatric cancer
- (2020) P. Jake Slavish et al. CANCER RESEARCH
- Rational Design and Evaluation of 6-(Pyrimidin-2-ylamino)-3,4-dihydroquinoxalin-2(1H)-ones as Polypharmacological Inhibitors of BET and Kinases
- (2020) Kaikai Lv et al. JOURNAL OF MEDICINAL CHEMISTRY
- The Design and Synthesis of a Highly Selective and In Vivo Capable Inhibitor of the Second Bromodomain (BD2) of the Bromodomain and Extra Terminal Domain (BET) Family of Proteins
- (2020) Alex Preston et al. JOURNAL OF MEDICINAL CHEMISTRY
- The Optimisation of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor
- (2020) Jonathan Thomas Seal et al. JOURNAL OF MEDICINAL CHEMISTRY
- GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins
- (2020) Robert J. Watson et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype
- (2020) Christopher R. Wellaway et al. JOURNAL OF MEDICINAL CHEMISTRY
- Design, synthesis, and biological evaluation of quinazolin-4(3H)-one derivatives co-targeting poly(ADP-ribose) polymerase-1 and bromodomain containing protein 4 for breast cancer therapy
- (2020) Xiaosa Chang et al. Acta Pharmaceutica Sinica B
- Selective N‐terminal BRD4 bromodomain inhibitors by targeting non‐conserved residues and structured water displacement
- (2020) William Charles Krause Pomerantz et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- BRD4 Interacts with GATA4 to Govern Mitochondrial Homeostasis in Adult Cardiomyocytes
- (2020) Arun Padmanabhan et al. CIRCULATION
- Inhibitors of bromodomain and extra‐terminal proteins for treating multiple human diseases
- (2020) Ewelina Kulikowski et al. MEDICINAL RESEARCH REVIEWS
- Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity
- (2019) Ellen Watts et al. JOURNAL OF MEDICINAL CHEMISTRY
- Inhibition of BRD4 suppresses the malignancy of breast cancer cells via regulation of Snail
- (2019) Linlin Lu et al. CELL DEATH AND DIFFERENTIATION
- Structure-guided drug design identifies a BRD4-selective small molecule that suppresses HIV
- (2019) Qingli Niu et al. JOURNAL OF CLINICAL INVESTIGATION
- Bromodomains: a new target class for drug development
- (2019) Andrea G. Cochran et al. NATURE REVIEWS DRUG DISCOVERY
- Emerging Screening Approaches in the Development of Nrf2–Keap1 Protein–Protein Interaction Inhibitors
- (2019) Chung-Hang Leung et al. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
- Systematically Mitigating the p38α Activity of Triazole-based BET Inhibitors
- (2019) Angela S. Carlson et al. ACS Medicinal Chemistry Letters
- Organization of Chromatin by Intrinsic and Regulated Phase Separation
- (2019) Bryan A. Gibson et al. CELL
- Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins
- (2019) Deheng Chen et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Systematic bromodomain protein screens identify homologous recombination and R-loop suppression pathways involved in genome integrity
- (2019) Jae Jin Kim et al. GENES & DEVELOPMENT
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- (2019) Yoel Rodríguez et al. PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS
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- (2019) Andrea Testa et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Discovery of Benzo[cd]indol-2(1H)-ones and Pyrrolo[4,3,2-de]quinolin-2(1H)-ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain with Potential High Efficiency against Acute Gouty Arthritis
- (2019) Fei Jiang et al. JOURNAL OF MEDICINAL CHEMISTRY
- AUTACs: Cargo-Specific Degraders Using Selective Autophagy
- (2019) Daiki Takahashi et al. MOLECULAR CELL
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- (2018) Chaoyang Sun et al. CANCER CELL
- Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation
- (2018) Zhiqing Liu et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain
- (2018) Robert P. Law et al. JOURNAL OF MEDICINAL CHEMISTRY
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- (2018) Chong Qin et al. JOURNAL OF MEDICINAL CHEMISTRY
- Plasticity in binding confers selectivity in ligand-induced protein degradation
- (2018) Radosław P. Nowak et al. Nature Chemical Biology
- BRD4 interacts with NIPBL and BRD4 is mutated in a Cornelia de Lange–like syndrome
- (2018) Gabrielle Olley et al. NATURE GENETICS
- BRD4 and MYC—clarifying regulatory specificity
- (2018) Arianna Sabò et al. SCIENCE
- Coactivator condensation at super-enhancers links phase separation and gene control
- (2018) Benjamin R. Sabari et al. SCIENCE
- BRD4 Promotes DNA Repair and Mediates the Formation of TMPRSS2-ERG Gene Rearrangements in Prostate Cancer
- (2018) Xiangyi Li et al. Cell Reports
- Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors
- (2018) Shuai Liu et al. JOURNAL OF MEDICINAL CHEMISTRY
- Molecular Basis for the N-Terminal Bromodomain and Extra Terminal (BET) Family Selectivity of a Dual Kinase-Bromodomain Inhibitor
- (2018) Anand Divakaran et al. JOURNAL OF MEDICINAL CHEMISTRY
- DUB3 Promotes BET Inhibitor Resistance and Cancer Progression by Deubiquitinating BRD4
- (2018) Xin Jin et al. MOLECULAR CELL
- Transcriptional addiction in cancer cells is mediated by YAP/TAZ through BRD4
- (2018) Francesca Zanconato et al. NATURE MEDICINE
- RNAs interact with BRD4 to promote enhanced chromatin engagement and transcription activation
- (2018) Homa Rahnamoun et al. NATURE STRUCTURAL & MOLECULAR BIOLOGY
- PLK1 stabilizes a MYC-dependent kinase network in aggressive B cell lymphomas
- (2018) Yuan Ren et al. JOURNAL OF CLINICAL INVESTIGATION
- BRD4 and Cancer: going beyond transcriptional regulation
- (2018) Benedetta Donati et al. Molecular Cancer
- Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains
- (2018) Jean-Philippe Lambert et al. MOLECULAR CELL
- Molecular dynamics simulations of macromolecular crystals
- (2018) David S. Cerutti et al. Wiley Interdisciplinary Reviews-Computational Molecular Science
- Design, synthesis and biological evaluation of novel indole derivatives as potential HDAC/BRD4 dual inhibitors and anti-leukemia agents
- (2018) Gaoliang Cheng et al. BIOORGANIC CHEMISTRY
- Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds
- (2017) Kwok-Ho Chan et al. JOURNAL OF MEDICINAL CHEMISTRY
- Drug Discovery Targeting Bromodomain-Containing Protein 4
- (2017) Zhiqing Liu et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression
- (2017) Bing Zhou et al. JOURNAL OF MEDICINAL CHEMISTRY
- BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells
- (2017) B Sun et al. LEUKEMIA
- Distinct Roles of Brd2 and Brd4 in Potentiating the Transcriptional Program for Th17 Cell Differentiation
- (2017) Ka Lung Cheung et al. MOLECULAR CELL
- Structural basis of PROTAC cooperative recognition for selective protein degradation
- (2017) Morgan S Gadd et al. Nature Chemical Biology
- 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
- 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
- Repression of BET activity sensitizes homologous recombination–proficient cancers to PARP inhibition
- (2017) Lu Yang et al. Science Translational Medicine
- Brd4 binds to active enhancers to control cell identity gene induction in adipogenesis and myogenesis
- (2017) Ji-Eun Lee et al. Nature Communications
- Computational protein structure refinement: almost there, yet still so far to go
- (2017) Michael Feig Wiley Interdisciplinary Reviews-Computational Molecular Science
- BRD4 regulates adiponectin gene induction by recruiting the P-TEFb complex to the transcribed region of the gene
- (2017) Naoko Sakurai et al. Scientific Reports
- Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors
- (2016) Zhimin Zhang et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- An Unexpected Chink in the Transcriptional Armor of Plasmacytoid Dendritic Neoplasms
- (2016) Maria Kleppe et al. CANCER CELL
- A Druggable TCF4- and BRD4-Dependent Transcriptional Network Sustains Malignancy in Blastic Plasmacytoid Dendritic Cell Neoplasm
- (2016) Michele Ceribelli et al. CANCER CELL
- Feedback Activation of Leukemia Inhibitory Factor Receptor Limits Response to Histone Deacetylase Inhibitors in Breast Cancer
- (2016) Hanlin Zeng et al. CANCER CELL
- Functional Genomic Landscape of Human Breast Cancer Drivers, Vulnerabilities, and Resistance
- (2016) Richard Marcotte et al. CELL
- Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET
- (2016) Luke W. Koblan et al. ChemMedChem
- AMPK–ULK1-Mediated Autophagy Confers Resistance to BET Inhibitor JQ1 in Acute Myeloid Leukemia Stem Cells
- (2016) Ji Eun Jang et al. CLINICAL CANCER RESEARCH
- Dual Kinase-Bromodomain Inhibitors in Anticancer Drug Discovery: A Structural and Pharmacological Perspective
- (2016) Luca Carlino et al. JOURNAL OF MEDICINAL CHEMISTRY
- Bet on drug resistance
- (2016) Jeff Settleman NATURE
- Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer
- (2016) Shaokun Shu et al. NATURE
- Induced protein degradation: an emerging drug discovery paradigm
- (2016) Ashton C. Lai et al. NATURE REVIEWS DRUG DISCOVERY
- 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
- PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer
- (2016) Kanak Raina et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- BRD4 is a histone acetyltransferase that evicts nucleosomes from chromatin
- (2016) Ballachanda N Devaiah et al. NATURE STRUCTURAL & MOLECULAR BIOLOGY
- BRD4 Phosphorylation Regulates HPV E2-Mediated Viral Transcription, Origin Replication, and Cellular MMP-9 Expression
- (2016) Shwu-Yuan Wu et al. Cell Reports
- Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
- (2015) Michael Zengerle et al. ACS Chemical Biology
- Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
- (2015) Jing Lu et al. CHEMISTRY & BIOLOGY
- 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
- Combined inhibition of BET family proteins and histone deacetylases as a potential epigenetics-based therapy for pancreatic ductal adenocarcinoma
- (2015) Pawel K Mazur et al. NATURE MEDICINE
- 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
- An iridium(iii)-based irreversible protein–protein interaction inhibitor of BRD4 as a potent anticancer agent
- (2015) Hai-Jing Zhong et al. Chemical Science
- GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1
- (2015) Krishan Kumar et al. Scientific Reports
- Disrupting the Interaction of BRD4 with Diacetylated Twist Suppresses Tumorigenesis in Basal-like Breast Cancer
- (2014) Jian Shi et al. CANCER CELL
- The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition
- (2014) Junwei Shi et al. MOLECULAR CELL
- Chromatin Reader Brd4 Functions in Ig Class Switching as a Repair Complex Adaptor of Nonhomologous End-Joining
- (2014) Andre Stanlie et al. MOLECULAR CELL
- Dual kinase-bromodomain inhibitors for rationally designed polypharmacology
- (2014) Pietro Ciceri et al. Nature Chemical Biology
- 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
- Inducible In Vivo Silencing of Brd4 Identifies Potential Toxicities of Sustained BET Protein Inhibition
- (2014) Jessica E. Bolden et al. Cell Reports
- Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains
- (2013) Mathew P. Martin et al. ACS Chemical Biology
- Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers
- (2013) Jakob Lovén et al. CELL
- Phospho Switch Triggers Brd4 Chromatin Binding and Activator Recruitment for Gene-Specific Targeting
- (2013) Shwu-Yuan Wu et al. MOLECULAR CELL
- Targeting protein–protein interactions as an anticancer strategy
- (2013) Andrei A. Ivanov et al. TRENDS IN PHARMACOLOGICAL SCIENCES
- 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
- Low-hanging fruit: targeting Brdt in the testes
- (2012) Jessica M Bryant et al. EMBO JOURNAL
- Peptoid ligands that bind selectively to phosphoproteins
- (2011) Di Cai et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- 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
- Brd4 Coactivates Transcriptional Activation of NF- B via Specific Binding to Acetylated RelA
- (2008) B. Huang et al. MOLECULAR AND CELLULAR BIOLOGY
- The Double Bromodomain Proteins Brd2 and Brd3 Couple Histone Acetylation to Transcription
- (2008) Gary LeRoy et al. MOLECULAR CELL
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