Pharmacological inhibition of bromodomain-containing proteins in inflammation. [PDF]
Cold Spring Harb Perspect Biol, 2014 Inflammation is associated with the activation of genes that contribute to immune defense and tissue repair. The bromodomain-containing proteins of the BET family, which recognize histone lysine acetylation, play a key role in the transcriptional control of inflammatory genes. Inhibition of BET proteins by the small-molecule inhibitor I-BET affects the
Schaefer U.
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Applying ⁸⁹Zr-Transferrin To Study the Pharmacology of Inhibitors to BET Bromodomain Containing Proteins. [PDF]
Mol Pharm, 2016 Chromatin modifying proteins are attractive drug targets in oncology, given the fundamental reliance of cancer on altered transcriptional activity. Multiple transcription factors can be impacted downstream of primary target inhibition, thus making it ...
Doran MG +8 more
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Design and synthesis of small molecule chemical probes for bromodomain-containing proteins
, 2014 Bromodomains (BRDs) are protein modules which bind to acetylated lysines on histones and transcriptional regulating proteins. BRD-containing proteins are involved in a large variety of critical cellular processes and their misregulation, or mutation of ...
Hay, Duncan A
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Novel Benzoisoxazoloazepine Inhibitors of Bromodomain-Containing Proteins. [PDF]
ACS Med Chem Lett, 2014 Rosse G.
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USP24 stabilizes bromodomain containing proteins to promote lung cancer malignancy. [PDF]
Sci Rep, 2020 AbstractBromodomain (BRD)-containing proteins are important for chromatin remodeling to regulate gene expression. In this study, we found that the deubiquitinase USP24 interacted with BRD through its C-terminus increased the levels of most BRD-containing proteins through increasing their protein stability by the removal of ubiquitin from Lys391/Lys400 ...
Wang SA +4 more
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Bromodomain-Containing Protein BRD4 Is Hyperphosphorylated in Mitosis [PDF]
Cancers, 2020 The epigenetic reader BRD4 binds acetylated histones and plays a central role in controlling cellular gene transcription and proliferation. Dysregulation of BRD4′s activity has been implicated in the pathogenesis of a wide variety of cancers. While blocking BRD4 interaction with acetylated histones using BET inhibitors (BETis) has been tested in ...
Ranran Wang +4 more
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Bromodomain-containing protein BRPF1 is a therapeutic target for liver cancer [PDF]
Communications Biology, 2021 AbstractEpigenetic deregulation plays an essential role in hepatocellular carcinoma (HCC) progression. Bromodomains are epigenetic “readers” of histone acetylation. Recently, bromodomain inhibitors have exhibited promising therapeutic potential for cancer treatment.
Carol Lai-Hung Cheng +10 more
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The BRPF1 bromodomain is a molecular reader of di-acetyllysine
Current Research in Structural Biology, 2020 Bromodomain-containing proteins are often part of chromatin-modifying complexes, and their activity can lead to altered expression of genes that drive cancer, inflammation and neurological disorders in humans.
Juliet O. Obi +10 more
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BET Bromodomain Inhibitors: Novel Design Strategies and Therapeutic Applications
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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Bromodomain-Containing Protein 4 [PDF]
Circulation Research, 2015 Rationale: Pulmonary arterial hypertension (PAH) is a vasculopathy characterized by enhanced pulmonary artery (PA) smooth muscle cell (PASMC) proliferation and suppressed apoptosis. Decreased expression of microRNA-204 has been associated to this phenotype.
Jolyane, Meloche +15 more
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