BET Bromodomain Inhibitors: Novel Design Strategies and Therapeutic Applications [PDF]
Molecules, 2023 The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer-related and immunity-associated genes.
Ross Larue, Kenneth Kin Wah To
exaly +4 more sources
BET bromodomain inhibitor HMBA synergizes with MEK inhibition in treatment of malignant glioma [PDF]
Epigenetics, 2021 (1) Background: BET bromodomain proteins regulate transcription by binding acetylated histones and attracting key factors for, e.g., transcriptional elongation.
Elisa Funck-Brentano +2 more
exaly +3 more sources
N-terminal BET bromodomain inhibitors disrupt a BRD4-p65 interaction and reduce inducible nitric oxide synthase transcription in pancreatic β-cells [PDF]
Frontiers in Endocrinology, 2022 Chronic inflammation of pancreatic islets is a key driver of β-cell damage that can lead to autoreactivity and the eventual onset of autoimmune diabetes (T1D).
Joshua A. Nord +8 more
doaj +2 more sources
Dissecting the Role of BET Bromodomain Proteins BRD2 and BRD4 in Human NK Cell Function [PDF]
Frontiers in Immunology, 2021 Natural killer (NK) cells are innate lymphocytes that play a pivotal role in the immune surveillance and elimination of transformed or virally infected cells.
Adam P. Cribbs +10 more
doaj +2 more sources
Immunogenicity of prostate cancer is augmented by BET bromodomain inhibition [PDF]
Journal for ImmunoTherapy of Cancer, 2019 Background Prostate cancer responds poorly to current immunotherapies. Epigenetic therapies such as BET Bromodomain inhibition can change the transcriptome of tumor cells, possibly making them more immunogenic and thus susceptible to immune targeting ...
Wendy Mao +8 more
doaj +2 more sources
BET bromodomain inhibition potentiates radiosensitivity in models of H3K27-altered diffuse midline glioma [PDF]
The Journal of Clinical InvestigationDiffuse midline glioma (DMG) H3K27-altered is one of the most malignant childhood cancers. Radiation therapy remains the only effective treatment yet provides a 5-year survival rate of only 1%.
Jun Watanabe +14 more
doaj +2 more sources
Genome-wide CRISPR-Cas9 screens identify mechanisms of BET bromodomain inhibitor sensitivity [PDF]
iScience, 2021 Summary: BET bromodomain inhibitors hold promise as therapeutic agents in diverse indications, but their clinical progression has been challenging and none have received regulatory approval.
David Estoppey +9 more
doaj +2 more sources
Stem Cell Research, 2016 Neural stem cells and progenitor cells (NPCs) are increasingly appreciated to hold great promise for regenerative medicine to treat CNS injuries and neurodegenerative diseases.
Rab K Prinjha +2 more
exaly +3 more sources
Cell Reports, 2017 Summary: BET inhibitors (BETi) target bromodomain-containing proteins and are currently being evaluated as anti-cancer agents. We find that maximal therapeutic effects of BETi in a Myc-driven B cell lymphoma model required an intact host immune system ...
Irina Sadovnik +2 more
exaly +3 more sources
Bromodomain and Extra-Terminal (BET) Domain Protein Inhibitors for Solid Tumor Cancers [PDF]
Journal of Immunotherapy and Precision Oncology, 2020 The bromodomain and extraterminal (BET) domain protein family is involved in the process of transcription of genetic information. The BET protein family includes BRD2, BRD3, BRD4, and bromodomain testis-specific protein.
Martin V. Nguyen +2 more
doaj +1 more source