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.
Kenneth K. W. To +3 more
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Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability. [PDF]
PLoS ONE, 2016 Lysine acetylation is an important epigenetic mark regulating gene transcription and chromatin structure. Acetylated lysine residues are specifically recognized by bromodomains, small protein interaction modules that read these modification in a sequence
Laura Lori +7 more
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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
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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
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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
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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
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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
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Inhibition of bromodomain and extra-terminal (BET) proteins increases NKG2D ligand MICA expression and sensitivity to NK cell-mediated cytotoxicity in multiple myeloma cells: role of cMYC-IRF4-miR-125b interplay [PDF]
Journal of Hematology & Oncology, 2016 Background Anti-cancer immune responses may contribute to the control of tumors after conventional chemotherapy, and different observations have indicated that chemotherapeutic agents can induce immune responses resulting in cancer cell death and immune ...
Maria Pia Abruzzese +13 more
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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 +3 more
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A Minireview on BET Inhibitors: Beyond Bromodomain Targeting
BiomedicinesBromodomain and extra-terminal domain (BET) proteins are epigenetic readers that recognize the histone acetylation code and play a critical role in regulating gene transcription.
Mikhail S. Iudin +4 more
doaj +3 more sources