BRD3 Regulates the Inflammatory and Stress Response in Rheumatoid Arthritis Synovial Fibroblasts [PDF]
Biomedicines, 2023 Background: Individual functions of members of the bromodomain (BRD) and extra-terminal (BET) protein family underlying the anti-inflammatory effects of BET inhibitors in rheumatoid arthritis (RA) are incompletely understood.
Matthias Brunner +2 more
exaly +8 more sources
Preparation data of the bromodomains BRD3(1), BRD3(2), BRD4(1), and BRPF1B and crystallization of BRD4(1)-inhibitor complexes [PDF]
Data in Brief, 2016 This article presents detailed purification procedures for the bromodomains BRD3(1), BRD3(2), BRD4(1), and BRPF1B. In addition we provide crystallization protocols for apo BRD4(1) and BRD4(1) in complex with numerous inhibitors.
Martin Hügle +11 more
doaj +5 more sources
BRD3 PROTAC degrader targets H3K18ac to alleviate retinal microglia-driven uveitis [PDF]
iScienceSummary: Uveitis is a sight-threatening intraocular inflammation in which the proinflammatory immune response driven by retinal microglia is a key contributor.
Zhi Zhang +10 more
doaj +4 more sources
BRD3 and BRD4 BET Bromodomain Proteins Differentially Regulate Skeletal Myogenesis
Scientific Reports, 2017 Myogenic differentiation proceeds through a highly coordinated cascade of gene activation that necessitates epigenomic changes in chromatin structure.
Thomas C. Roberts +7 more
doaj +6 more sources
Recruitment of Brd3 and Brd4 to acetylated chromatin is essential for proinflammatory cytokine-induced matrix-degrading enzyme expression [PDF]
Journal of Orthopaedic Surgery and Research, 2019 Background Proinflammatory cytokines, which can upregulate the expression of matrix-degrading enzymes in chondrocytes, play important roles in the development of osteoarthritis.
Jin Dai +11 more
doaj +4 more sources
Tumor suppressive role of the epigenetic master regulator BRD3 in colorectal cancer [PDF]
Cancer ScienceAbstractBromodomain and extraterminal domain (BET) family proteins are epigenetic master regulators of gene expression via recognition of acetylated histones and recruitment of transcription factors and co‐activators to chromatin. Hence, BET family proteins have emerged as promising therapeutic targets in cancer.
Masahiro Hashimoto +2 more
exaly +4 more sources
Targeting BRD3 eradicates nuclear TYRO3-induced colorectal cancer metastasis
Science Advances, 2023 Metastasis is the main cause of death in many cancers including colorectal cancer (CRC); however, the underlying mechanisms responsible for metastatic progression remain largely unknown. We found that nuclear TYRO3 receptor tyrosine kinase is a strong predictor of poor overall survival in patients with CRC.
Pei-Ling Hsu, Yen-An Tang, Bo-Wen Lin
exaly +3 more sources
The Double Bromodomain Proteins Brd2 and Brd3 Couple Histone Acetylation to Transcription [PDF]
Molecular Cell, 2008 Posttranslational histone modifications are crucial for the modulation of chromatin structure and regulation of transcription. Bromodomains present in many chromatin-associated proteins recognize acetylated lysines in the unstructured N-terminal regions of histones.
Gary Leroy, S J Flint
exaly +3 more sources
Deep learning-guided discovery of selective JAK2-JH2 allosteric inhibitors: integration of MLP predictive modeling, BREED-based library design, and computational validation [PDF]
Frontiers in ChemistryThe JAK2 pseudokinase domain (JH2) is an important therapeutic target in hematologic and oncologic diseases, motivating the search for selective allosteric inhibitors.
Mebarka Ouassaf +6 more
doaj +2 more sources
BET family BRD3 initiates DSB-induced chromatin remodeling with TIP60 to promote R-loop-mediated HR
Cell ReportsSummary: Mechanisms for genome stability in actively transcribed regions are essential for cellular homeostasis; however, these mechanisms are poorly understood. Herein, we identify the bromodomain and extraterminal domain (BET) family BRD3 as the genome
Ayako Ui
exaly +3 more sources