4.5 Review

BET bromodomain inhibitors

Related references

Note: Only part of the references are listed.
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)

Review Oncology

Bromodomain and extra-terminal inhibitors-A consensus prioritisation after the Paediatric Strategy Forum for medicinal product development of epigenetic modifiers in children-ACCELERATE

Andrew D. J. Pearson et al.

Summary: BET inhibitors have potential roles in pediatric oncology, but further research and evaluation are needed. Clinical assessment in children should be prioritized based on specific drugs. Collaborative efforts can improve development efficiency and maximize benefits for pediatric patients.

EUROPEAN JOURNAL OF CANCER (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 Chemistry, Medicinal

4-Methyl-1,2,3-Triazoles as N-Acetyl-Lysine Mimics Afford Potent BET Bromodomain Inhibitors with Improved Selectivity

Huarui Cui et al.

Summary: The BET protein family recognizes acetylated lysines using two N-terminal bromodomains, and these interactions are therapeutic targets for BET-related diseases. A structure-activity relationship study of triazole-based inhibitors improved affinity, D1 selectivity, and microsomal stability by targeting specific residues on BRD4 D1. Lead inhibitors DW34 and 26 showed promising activity in suppressing c-Myc expression and downregulating IL-8, suggesting their potential as new leads for investigating anticancer and anti-inflammatory activity of BET proteins.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Medicinal

Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression

Katherine L. Jones et al.

Summary: This study details the optimization process of the in vivo tool molecule I-BET151 towards I-BET282E, a molecule with properties suitable for clinical progression, in order to reduce the risk of compound attrition due to related toxicity findings.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Oncology

Paradigm shift: combination BET and JAK inhibition in myelofibrosis

John Mascarenhas et al.

LEUKEMIA (2021)

Article Chemistry, Multidisciplinary

Potent Dual BET/HDAC Inhibitors for Efficient Treatment of Pancreatic Cancer

Shipeng He et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2020)

Article Multidisciplinary Sciences

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

Emily J. Faivre et al.

NATURE (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)

Review Biotechnology & Applied Microbiology

Bromodomains: a new target class for drug development

Andrea G. Cochran et al.

NATURE REVIEWS DRUG DISCOVERY (2019)

Article Multidisciplinary Sciences

Spatially constrained tandem bromodomain inhibition bolsters sustained repression of BRD4 transcriptional activity for TNBC cell growth

Chunyan Ren et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2018)

Article Chemistry, Medicinal

Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor

Jianping Hu et al.

EUROPEAN 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

Design and characterization of bivalent BET inhibitors

Minoru Tanaka et al.

NATURE CHEMICAL BIOLOGY (2016)

Article Biochemistry & Molecular Biology

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

Jing Lu et al.

CHEMISTRY & BIOLOGY (2015)

Article Chemistry, Medicinal

Fragment-Based Drug Discovery of 2-Thiazolidinones as BRD4 Inhibitors: 2. Structure-Based Optimization

Lele Zhao et al.

JOURNAL OF MEDICINAL CHEMISTRY (2015)

Article Multidisciplinary Sciences

Phthalimide conjugation as a strategy for in vivo target protein degradation

Georg E. Winter et al.

SCIENCE (2015)

Article Chemistry, Medicinal

BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536

Lijia Chen et al.

ACS MEDICINAL CHEMISTRY LETTERS (2015)

Article Biochemistry & Molecular Biology

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors

Stuart W. J. Ember et al.

ACS CHEMICAL BIOLOGY (2014)

Article Biochemistry & Molecular Biology

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

Pietro Ciceri et al.

NATURE CHEMICAL BIOLOGY (2014)

Article Biochemistry & Molecular Biology

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

Jakob Loven et al.

Article Chemistry, Medicinal

Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening

Lewis R. Vidler et al.

JOURNAL OF MEDICINAL CHEMISTRY (2013)

Article Multidisciplinary Sciences

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

Sarah Picaud et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2013)

Article Chemistry, Medicinal

Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors

Victor S. Gehling et al.

ACS MEDICINAL CHEMISTRY LETTERS (2013)

Article Biochemistry & Molecular Biology

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

Panagis Filippakopoulos et al.

Article Chemistry, Medicinal

Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites

Lewis R. Vidler et al.

JOURNAL OF MEDICINAL CHEMISTRY (2012)

Article Biochemistry & Molecular Biology

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

Jake E. Delmore et al.

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 Multidisciplinary Sciences

Identification of a Primary Target of Thalidomide Teratogenicity

Takumi Ito et al.

SCIENCE (2010)

Article Chemistry, Multidisciplinary

Selective small molecules blocking HIV-1 Tat and coactivator PCAF association

L Zeng et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2005)