Progress in the development of domain selective inhibitors of the bromo and extra terminal domain family (BET) proteins.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113853
Abstract: Dysfunction of the bromo and extra terminal domain (BET) family proteins is associated with many human diseases, therefore the BET family proteins have been considered as promising targets for drug development. Numerous small molecular compounds… read more here.
Keywords: extra terminal; bromo extra; family; domain ... 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-Based Discovery and Optimization of Furo[3,2-c]pyridin-4(5H)-one Derivatives as Potent and Second Bromodomain (BD2)-Selective Bromo and Extra Terminal Domain (BET) Inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00100
Abstract: Pan-bromodomain and extra terminal (Pan-BET) inhibitors show profound efficacy but exhibit pharmacology-driven toxicities in clinical trials. The development of domain-selective BET inhibitors to separate efficacy and toxicity is urgently needed. Herein, we report a series… read more here.
Keywords: furo pyridin; extra terminal; bd2; bet inhibitors ... 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
Ustilago maydis telomere protein Pot1 harbors an extra N-terminal OB fold and regulates homology-directed DNA repair factors in a dichotomous and context-dependent manner
Sign Up to like & getrecommendations! Published in 2022 at "PLoS Genetics"
DOI: 10.1371/journal.pgen.1010182
Abstract: The telomere G-strand binding protein Pot1 plays multifaceted roles in telomere maintenance and protection. We examined the structure and activities of Pot1 in Ustilago maydis, a fungal model that recapitulates key features of mammalian telomere… read more here.
Keywords: ustilago maydis; protein pot1; extra terminal; terminal fold ... 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
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
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