4.4 Review

Annual Review of Cancer Biology Targeting BET Bromodomains in Cancer

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Oncology

Overview of Myeloproliferative Neoplasms History, Pathogenesis, Diagnostic Criteria, and Complications

Douglas Tremblay et al.

HEMATOLOGY-ONCOLOGY CLINICS OF NORTH AMERICA (2021)

Review Biochemistry & Molecular Biology

Supercharging BRD4 with NUT in carcinoma

Kyle P. Eagen et al.

Summary: NUT carcinoma is an extremely aggressive squamous cancer driven by the BRD4-NUT fusion oncoprotein, offering potential therapeutic targets such as BET inhibitors. The BRD4-NUT complex recruits and activates histone acetyltransferase p300, forming hyperacetylated chromatin foci known as megadomains that regulate stem cell-related transcription factors. These megadomains also create a novel nuclear sub-compartment, called subcompartment M, with implications for 3D genome organization and gene regulation. Leveraging knowledge of BRD4-NUT function has led to the development of targeted therapies.

ONCOGENE (2021)

Review Virology

Modulation of BRD4 in HIV epigenetic regulation: implications for finding an HIV cure

Edrous Alamer et al.

Summary: Following reverse transcription, HIV viral DNA integrates into host cell genomes to establish a stable latent infection. BRD4, an epigenetic reader, plays a crucial role in controlling gene expression including HIV. Recent studies suggest that BRD4's effects on HIV transcription might vary depending on the partner proteins or pathways it interacts with.

RETROVIROLOGY (2021)

Review Pharmacology & Pharmacy

Safety and Efficacy of Bromodomain and Extra-Terminal Inhibitors for the Treatment of Hematological Malignancies and Solid Tumors: A Systematic Study of Clinical Trials

Yanli Sun et al.

Summary: The upregulated expression of BET proteins is closely related to hematological malignancies and solid tumors. Ten BET inhibitors currently in clinical trials showed exposure-dependent thrombocytopenia, and further efforts are needed to explore optimal dosing schemes for maximizing their efficacy.META_DESCRIPTION

FRONTIERS IN PHARMACOLOGY (2021)

Article Chemistry, Medicinal

Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development

Pan Tang et al.

Summary: BET proteins regulate chromatin dynamics, cellular processes, and disease progression by binding acetylated lysine residues in histones and nonhistone proteins, making them a promising strategy for treating malignant tumors and chronic inflammation. However, the clinical efficacy of current BET inhibitors is limited, leading to the development of new technologies to improve outcomes and minimize side effects.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Medicinal

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

Peter S. Dragovich et al.

Summary: This study explores the use of antibody-drug conjugates as delivery vehicles to improve the bioavailability and anticancer activity of proteolysis-targeting chimeras. Results demonstrate that these conjugates can have antigen-dependent effects on prostate cancer cells.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Medicinal

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy

Peter S. Dragovich et al.

Summary: Heterobifunctional compounds that direct the ubiquitination of intracellular proteins have the potential to transform medicinal chemistry. This report focuses on exploring antibody-drug conjugates incorporating BRD4-targeting chimeric degrader entities, which showed potent BRD4 degradation and antiproliferation activities in cell-based experiments, as well as strong antitumor efficacy in mouse xenograft assessments.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Medicinal

Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors

Helen E. Aylott et al.

Summary: This study successfully reduced the genotoxicity risk of GSK046 by replacing the acetamide functionality with a heterocyclic ring, and identified potent, selective, and bioavailable compounds through a structure-based drug design approach.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Review Oncology

Achieving clinical success with BET inhibitors as anti-cancer agents

Tatiana Shorstova et al.

Summary: Transcriptional upregulation of oncogenes drives tumor progression, and targeting BET proteins with inhibitors has shown promise in suppressing oncogenic networks in tumors. Understanding the biology of BET proteins, designing better BET inhibitors, and incorporating BET inhibitors into combination therapies can enhance their efficacy in clinical settings.

BRITISH JOURNAL OF CANCER (2021)

Article Biochemistry & Molecular Biology

BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection

Richard J. Mills et al.

Summary: Cardiac injury and dysfunction in COVID-19 patients increase mortality risk. An inflammatory cytokine-storm can induce diastolic dysfunction, but BET inhibitors show promise in preventing cardiac damage and dysfunction induced by the virus.
Article Cardiac & Cardiovascular Systems

Relation of insulin treatment for type 2 diabetes to the risk of major adverse cardiovascular events after acute coronary syndrome: an analysis of the BETonMACE randomized clinical trial

Gregory G. Schwartz et al.

Summary: In patients with type 2 diabetes, low HDL cholesterol, and ACS, insulin treatment is associated with a higher risk of major adverse cardiovascular events compared to those not treated with insulin. Despite utilization of evidence-based treatments, the incidence of MACE remains elevated in insulin-treated patients.

CARDIOVASCULAR DIABETOLOGY (2021)

Review Oncology

Hypertranscription and replication stress in cancer

Akhil Bowry et al.

Summary: Studies have shown that oncogenic signaling and targeted cancer treatments can increase global transcription activity, leading to replication stress. However, research on this hypertranscription phenomenon is often neglected compared to other causes of replication stress in cancer.

TRENDS IN CANCER (2021)

Article Chemistry, Medicinal

Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

Thomas H. Pillow et al.

CHEMMEDCHEM (2020)

Article Multidisciplinary Sciences

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

Emily J. Faivre et al.

NATURE (2020)

Article Biochemistry & Molecular Biology

Covalent-Fragment Screening of BRD4 Identifies a Ligandable Site Orthogonal to the Acetyl-Lysine Binding Sites

Michael D. Olp et al.

ACS CHEMICAL BIOLOGY (2020)

Review Biochemistry & Molecular Biology

Domain-selective targeting of BET proteins in cancer and immunological diseases

Massimo Petretich et al.

CURRENT OPINION IN CHEMICAL BIOLOGY (2020)

Review Immunology

Bromodomain Inhibitors as Therapeutics for Herpesvirus-Related Disease: All BETs Are Off?

Ian J. Groves et al.

FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY (2020)

Article Chemistry, Medicinal

GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins

Robert J. Watson et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

Article Chemistry, Medicinal

GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family

Alex Preston et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

Review Biotechnology & Applied Microbiology

Bromodomains: a new target class for drug development

Andrea G. Cochran et al.

NATURE REVIEWS DRUG DISCOVERY (2019)

Meeting Abstract Oncology

GNE-0011, a novel monovalent BRD4 degrader

Robert A. Blake

CANCER RESEARCH (2019)

Article Chemistry, Medicinal

Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation

Zhiqing Liu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Biochemistry & Molecular Biology

Plasticity in binding confers selectivity in ligand-induced protein degradation

Radoslaw P. Nowak et al.

NATURE CHEMICAL BIOLOGY (2018)

Article Biochemistry & Molecular Biology

DUB3 Promotes BET Inhibitor Resistance and Cancer Progression by Deubiquitinating BRD4

Xin Jin et al.

MOLECULAR CELL (2018)

Article Chemistry, Medicinal

Drug Discovery Targeting Bromodomain-Containing Protein 4

Zhiqing Liu et al.

JOURNAL OF MEDICINAL CHEMISTRY (2017)

Article Biochemistry & Molecular Biology

Structural basis of PROTAC cooperative recognition for selective protein degradation

Morgan S. Gadd et al.

NATURE CHEMICAL BIOLOGY (2017)

Article Biochemistry & Molecular Biology

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

Xiangpeng Dai et al.

NATURE MEDICINE (2017)

Article Multidisciplinary Sciences

Click chemistry enables preclinical evaluation of targeted epigenetic therapies

Dean S. Tyler et al.

SCIENCE (2017)

Review Hematology

Management of myelofibrosis: JAK inhibition and beyond

Maximilian Stahl et al.

EXPERT REVIEW OF HEMATOLOGY (2017)

Article Medicine, Research & Experimental

Targeting Cancer Cells with BET Bromodomain Inhibitors

Yali Xu et al.

COLD SPRING HARBOR PERSPECTIVES IN MEDICINE (2017)

Review Oncology

Novel Therapies for Myelofibrosis

Kristen Pettit et al.

CURRENT HEMATOLOGIC MALIGNANCY REPORTS (2017)

Review Oncology

BET inhibitors: a novel epigenetic approach

D. B. Doroshow et al.

ANNALS OF ONCOLOGY (2017)

Review Biochemistry & Molecular Biology

The Bromodomain and Extra-Terminal Domain (BET) Family: Functional Anatomy of BET Paralogous Proteins

Yasushi Taniguchi

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2016)

Article Biochemistry & Molecular Biology

Potent and selective bivalent inhibitors of BET bromodomains

Michael J. Waring et al.

NATURE CHEMICAL BIOLOGY (2016)

Article Biochemistry & Molecular Biology

Design and characterization of bivalent BET inhibitors

Minoru Tanaka et al.

NATURE CHEMICAL BIOLOGY (2016)

Review Biotechnology & Applied Microbiology

Epigenetic drug discovery: breaking through the immune barrier

David F. Tough et al.

NATURE REVIEWS DRUG DISCOVERY (2016)

Review Neurosciences

Bromodomains: Translating the words of lysine acetylation into myelin injury and repair

Achilles Ntranos et al.

NEUROSCIENCE LETTERS (2016)

Article Multidisciplinary Sciences

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

Kanak Raina et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2016)

Article Biochemistry & Molecular Biology

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

Michael Zengerle et al.

ACS CHEMICAL BIOLOGY (2015)

Article Multidisciplinary Sciences

Transcriptional plasticity promotes primary and acquired resistance to BET inhibition

Philipp Rathert et al.

NATURE (2015)

Article Multidisciplinary Sciences

BET inhibitor resistance emerges from leukaemia stem cells

Chun Yew Fong et al.

NATURE (2015)

Article Multidisciplinary Sciences

BRD4 is a novel therapeutic target for liver fibrosis

Ning Ding et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2015)

Article Biochemistry & Molecular Biology

Regulation of NO Synthesis, Local Inflammation, and Innate Immunity to Pathogens by BET Family Proteins

Sebastian Wienerroither et al.

MOLECULAR AND CELLULAR BIOLOGY (2014)

Article Multidisciplinary Sciences

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

Irfan A. Asangani et al.

NATURE (2014)

Review Biotechnology & Applied Microbiology

Targeting bromodomains: epigenetic readers of lysine acetylation

Panagis Filippakopoulos et al.

NATURE REVIEWS DRUG DISCOVERY (2014)

Article Multidisciplinary Sciences

Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors

Michele Ceribelli et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2014)

Article Biochemistry & Molecular Biology

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

Jakob Loven et al.

Article Biochemistry & Molecular Biology

Integrative Analysis of Complex Cancer Genomics and Clinical Profiles Using the cBioPortal

Jianjiong Gao et al.

SCIENCE SIGNALING (2013)

Article Biochemistry & Molecular Biology

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

Panagis Filippakopoulos et al.

Article Multidisciplinary Sciences

Functional genomics identifies therapeutic targets for MYC-driven cancer

Masafumi Toyoshima et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2012)

Article Biochemistry & Molecular Biology

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

Jake E. Delmore et al.

Article Multidisciplinary Sciences

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

Johannes Zuber et al.

NATURE (2011)

Article Multidisciplinary Sciences

Targeting MYC dependence in cancer by inhibiting BET bromodomains

Jennifer A. Mertz et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2011)

Article Multidisciplinary Sciences

Suppression of inflammation by a synthetic histone mimic

Edwige Nicodeme et al.

NATURE (2010)

Article Multidisciplinary Sciences

Selective inhibition of BET bromodomains

Panagis Filippakopoulos et al.

NATURE (2010)

Article Anatomy & Morphology

Double Bromodomain-Containing Gene Brd2 Is Essential for Embryonic Development in Mouse

Enyuan Shang et al.

DEVELOPMENTAL DYNAMICS (2009)

Article Biochemistry & Molecular Biology

The double bromodomain proteins Brd2 and Brd3 couple histone acetylation to transcription

Gary LeRoy et al.

MOLECULAR CELL (2008)

Review Biochemistry & Molecular Biology

Structure and acetyl-lysine recognition of the bromodomain

S. Mujtaba et al.

ONCOGENE (2007)

Article Biochemistry & Molecular Biology

Growth and early postimplantation defects in mice deficient for the bromodomain-containing protein Brd4

D Houzelstein et al.

MOLECULAR AND CELLULAR BIOLOGY (2002)