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Published in 2019 at "American Journal of Cardiovascular Drugs"
DOI: 10.1007/s40256-018-00315-3
Abstract: Bromodomain and extra-terminal (BET) inhibitors, acting via epigenetic mechanisms, have been developed recently as potential new treatments for cancer, including prostate cancer, and inflammatory conditions. Some BET inhibitors, such as RVX-208, also raise high-density lipoprotein…
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Keywords:
disease;
bromodomain extra;
rvx 208;
cardiovascular disease ... See more keywords
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Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01323
Abstract: To better understand the role of bromodomain and extra-terminal domain (BET) proteins in epigenetic mechanisms, we developed a series of thienodiazepine-based derivatives and identified two compounds, 3a and 6a, as potent BET inhibitors. Further in…
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Keywords:
extra terminal;
terminal domain;
imaging probes;
positron emission ... See more keywords
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Published in 2018 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.6b01816
Abstract: The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are considered to…
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Keywords:
extra terminal;
bet proteins;
small molecule;
bet ... See more keywords
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Published in 2022 at "Chemical communications"
DOI: 10.1039/d2cc03785h
Abstract: The two tandem bromodomains of BET (bromodomain and extra-terminal domain) proteins (BD1 and BD2) may play distinct and critical roles in neurological diseases. To better understand the underlying mechanisms of the BD1 bromodomain and facilitate…
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Keywords:
positron emission;
bd1 bromodomain;
bromodomain extra;
terminal domain ... See more keywords
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Published in 2022 at "Frontiers in Cell and Developmental Biology"
DOI: 10.3389/fcell.2022.1021820
Abstract: Bromodomain and extra-terminal domain (BET) family proteins play important roles in regulating the expression of multiple proto-oncogenes by recognizing acetylation of histones and non-histone proteins including transcription factors, which subsequently promote tumor cell proliferation, survival,…
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Keywords:
tumorigenesis;
bromodomain extra;
targeting bromodomain;
extra terminal ... See more keywords
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Published in 2022 at "Pharmaceuticals"
DOI: 10.3390/ph15060665
Abstract: Pediatric brain tumors have surpassed leukemia as the leading cause of cancer-related death in children. Several landmark studies from the last two decades have shown that many pediatric brain tumors are driven by epigenetic dysregulation…
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Keywords:
pediatric brain;
brain tumors;
bromodomain extra;
brain ... See more keywords
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Published in 2022 at "Pharmaceuticals"
DOI: 10.3390/ph15081032
Abstract: BET proteins, which recognize and bind to acetylated histones, play a key role in transcriptional regulation. The development of chemical BET inhibitors in 2010 greatly facilitated the study of these proteins. BETs play crucial roles…
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Keywords:
bet;
roles bromodomain;
bromodomain extra;
metabolic signaling ... See more keywords
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Published in 2022 at "World Journal of Gastrointestinal Oncology"
DOI: 10.4251/wjgo.v14.i1.75
Abstract: Gastrointestinal (GI) cancers, including colorectal cancer, pancreatic cancer, liver cancer and gastric cancer, are severe social burdens due to high incidence and mortality rates. Bromodomain and extra-terminal (BET) proteins are epigenetic readers consisting of four…
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Keywords:
gastrointestinal cancers;
bromodomain extra;
extra terminal;
bet proteins ... See more keywords