An optimized BRD4 inhibitor effectively eliminates NF-κB-driven triple-negative breast cancer cells

Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease

(2021) Kamakoti P. Bhat et al.   NATURE REVIEWS DRUG DISCOVERY

A 7-methoxybicoumarin derivative selectively inhibits BRD4 BD2 for anti-melanoma therapy

(2020) Guan-Jun Yang et al.   INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Structure-Based Discovery of a Selective KDM5A Inhibitor that Exhibits Anti-Cancer Activity via Inducing Cell Cycle Arrest and Senescence in Breast Cancer Cell Lines

(2019) Guan-Jun Yang et al.   Cancers

Emerging roles of and therapeutic strategies targeting BRD4 in cancer

(2019) Mary E. White et al.   CELLULAR IMMUNOLOGY

Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer

(2019) María del Mar Noblejas-López et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

BET protein targeting suppresses the PD-1/PD-L1 pathway in triple-negative breast cancer and elicits anti-tumor immune response

(2019) Guillaume P. Andrieu et al.   CANCER LETTERS

Selective Inhibition of Lysine-Specific Demethylase 5A (KDM5A) Using a Rhodium(III) Complex for Triple-Negative Breast Cancer Therapy

(2018) Guan-Jun Yang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Design, synthesis and biological evaluation of benzo[ cd ]indol-2(1 H )-ones derivatives as BRD4 inhibitors

(2018) Yuxin Feng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Selective Antagonists of the Bronchiolar Epithelial NF-κB-Bromodomain-Containing Protein 4 Pathway in Viral-Induced Airway Inflammation

(2018) Bing Tian et al.   Cell Reports

Gain of UBE2D1 facilitates hepatocellular carcinoma progression and is associated with DNA damage caused by continuous IL-6

(2018) Chuanchuan Zhou et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

STAT3/NF-κB-Regulated Lentiviral TK/GCV Suicide Gene Therapy for Cisplatin-Resistant Triple-Negative Breast Cancer

(2017) Wei-Ying Kuo et al.   Theranostics

BRD4 mediates NF-κB-dependent epithelial-mesenchymal transition and pulmonary fibrosis via transcriptional elongation

(2016) Bing Tian et al.   AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY

Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins

(2016) Brigitt Raux et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2016) Shaokun Shu et al.   NATURE

Triple-negative breast cancer: challenges and opportunities of a heterogeneous disease

(2016) Giampaolo Bianchini et al.   Nature Reviews Clinical Oncology

Synergistic activity of BET protein antagonist-based combinations in mantle cell lymphoma cells sensitive or resistant to ibrutinib

(2015) B. Sun et al.   BLOOD

Molecular characterization and functional analysis of a novel C-type lectin receptor-like gene from a teleost fish, Plecoglossus altivelis

(2015) Guan-Jun Yang et al.   FISH & SHELLFISH IMMUNOLOGY

Acute TNF-induced repression of cell identity genes is mediated by NFκB-directed redistribution of cofactors from super-enhancers

(2015) Søren Fisker Schmidt et al.   GENOME RESEARCH

IL-10 disrupts the Brd4-docking sites to inhibit LPS-induced CXCL8 and TNF-α expression in monocytes: Implications for chronic obstructive pulmonary disease

(2015) Monica Castellucci et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

BET Bromodomains Regulate Transforming Growth Factor-β-induced Proliferation and Cytokine Release in Asthmatic Airway Smooth Muscle

(2015) Mark M. Perry et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The TNFα converting enzyme (TACE) from ayu (Plecoglossus altivelis) exhibits TNFα shedding activity

(2015) Xin-Jiang Lu et al.   MOLECULAR IMMUNOLOGY

An iridium(iii)-based irreversible protein–protein interaction inhibitor of BRD4 as a potent anticancer agent

(2015) Hai-Jing Zhong et al.   Chemical Science

NF-κB Directs Dynamic Super Enhancer Formation in Inflammation and Atherogenesis

(2014) Jonathan D. Brown 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

Re-Place Your BETs: The Dynamics of Super Enhancers

(2014) Paulo P. Amaral et al.   MOLECULAR CELL

Brd4 is on the move during inflammation

(2014) Yali Xu et al.   TRENDS IN CELL BIOLOGY

Identification of a natural product-like STAT3 dimerization inhibitor by structure-based virtual screening

(2014) L-J Liu et al.   Cell Death & Disease

The bromodomain protein Brd4 insulates chromatin from DNA damage signalling

(2013) Scott R. Floyd et al.   NATURE

Brd4 maintains constitutively active NF-κB in cancer cells by binding to acetylated RelA

(2013) Z Zou et al.   ONCOGENE

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

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

(2011) Jake E. Delmore et al.   CELL

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Persistently Activated Stat3 Maintains Constitutive NF-κB Activity in Tumors

(2009) Heehyoung Lee et al.   CANCER CELL