How Might Bromodomain and Extra-Terminal (BET) Inhibitors Operate in Cardiovascular Disease?
Sign Up to like & getrecommendations! 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… read more here.
Keywords: disease; bromodomain extra; rvx 208; cardiovascular disease ... See more keywords
Design, Synthesis, and Evaluation of Thienodiazepine Derivatives as Positron Emission Tomography Imaging Probes for Bromodomain and Extra-Terminal Domain Family Proteins.
Sign Up to like & getrecommendations! 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… read more here.
Keywords: extra terminal; terminal domain; imaging probes; positron emission ... See more keywords
Structure- and Property-Based Optimization of Efficient Pan-Bromodomain and Extra Terminal Inhibitors to Identify Oral and Intravenous Candidate I-BET787.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c00959
Abstract: The bromodomain and extra terminal (BET) family of bromodomain-containing proteins are important epigenetic regulators that elicit their effect through binding histone tail N-acetyl lysine (KAc) post-translational modifications. Recognition of such markers has been implicated in… read more here.
Keywords: chemistry; bromodomain extra; based optimization; structure property ... See more keywords
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression
Sign Up to like & getrecommendations! 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… read more here.
Keywords: extra terminal; bet proteins; small molecule; bet ... See more keywords
A positron emission tomography imaging probe selectively targeting the BD1 bromodomain and extra-terminal domain.
Sign Up to like & getrecommendations! 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… read more here.
Keywords: positron emission; bd1 bromodomain; bromodomain extra; terminal domain ... See more keywords
Targeting bromodomain and extra-terminal proteins to inhibit neuroblastoma tumorigenesis through regulating MYCN
Sign Up to like & getrecommendations! 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,… read more here.
Keywords: tumorigenesis; bromodomain extra; targeting bromodomain; extra terminal ... See more keywords
Therapeutic Potential of Bromodomain and Extra-Terminal Domain Inhibitors for Synovial Sarcoma Cells
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DOI: 10.3390/cancers16061125
Abstract: Simple Summary Synovial sarcoma, a rare type of soft-tissue sarcoma, currently lacks efficacious anticancer therapies. This sarcoma is characterized by the SS18-SSX fusion gene, which plays a pivotal role in epigenetic regulation. Our study centered… read more here.
Keywords: bromodomain extra; ss18 ssx; synovial sarcoma; sarcoma ... See more keywords
Bromodomain and Extra-Terminal Protein Inhibitors: Biologic Insights and Therapeutic Potential in Pediatric Brain Tumors
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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… read more here.
Keywords: pediatric brain; brain tumors; bromodomain extra; brain ... See more keywords
Roles of Bromodomain Extra Terminal Proteins in Metabolic Signaling and Diseases
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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… read more here.
Keywords: bet; roles bromodomain; bromodomain extra; metabolic signaling ... See more keywords
Development of a PET Probe Targeting Bromodomain and Extra-Terminal Proteins for In Vitro and In Vivo Visualization
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DOI: 10.3390/ph17121670
Abstract: Background: Bromodomain and extra-terminal (BET) proteins are critical regulators of gene transcription, as they recognize acetylated lysine residues. The BD1 bromodomain of BRD4, a member of the BET family, has emerged as a promising therapeutic… read more here.
Keywords: 11c yl10; bromodomain extra; bd1 bromodomain; bromodomain ... See more keywords
Bromodomain and extra-terminal inhibitors emerge as potential therapeutic avenues for gastrointestinal cancers
Sign Up to like & getrecommendations! 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… read more here.
Keywords: gastrointestinal cancers; bromodomain extra; extra terminal; bet proteins ... See more keywords