Rationally designed chimeric PI3K-BET bromodomain inhibitors elicit curative responses in MYC-driven lymphoma. [PDF]
Proc Natl Acad Sci U S A, 2023 Oh DH +16 more
europepmc +1 more source
BET Bromodomain Degradation Disrupts Function but Not 3D Formation of RNA Pol2 Clusters. [PDF]
Pharmaceuticals (Basel), 2023 Chin DH +13 more
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BET Bromodomain as a Target of Epigenetic Therapy
CHEMICAL & PHARMACEUTICAL BULLETIN, 2016 Acetylation of histone is a key epigenetic modification, and contributes to many DNA-dependent cellular processes. The bromodomain structure, which consists of approximately 110 amino acid residues, serves as a 'reader' that recognizes acetylated lysine in histones, leading to recruitment of positive transcriptional elongation factor b (P-TEFb), and ...
openaire +3 more sources
Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment In Vitro and In Vivo. [PDF]
Mol Cancer Ther, 2023 Jonchere B +14 more
europepmc +1 more source
Journal of InflammationBromodomain-containing protein 4 (BRD4), a key member of the bromodomain and extra-terminal (BET) family, plays a critical role in regulating gene expression as an epigenetic reader.
Rachele Frascatani +3 more
doaj +1 more source
Alternative Mechanisms for DNA Engagement by BET Bromodomain-Containing Proteins. [PDF]
Biochemistry, 2022 Kalra P +4 more
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Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors. [PDF]
J Med Chem, 2021 Karim RM +9 more
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Sensitization of Resistant Cells with a BET Bromodomain Inhibitor in a Cell Culture Model of Deep Intrinsic Resistance in Breast Cancer. [PDF]
Cancers (Basel), 2023 Singh B +7 more
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Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity. [PDF]
J Med Chem, 2022 Guan X +7 more
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