A Chemical Screen Identifies Compounds Limiting the Toxicity of C9ORF72 Dipeptide Repeats.
Sign Up to like & getrecommendations! Published in 2019 at "Cell chemical biology"
DOI: 10.1016/j.chembiol.2018.10.020
Abstract: The expansion of GGGGCC repeats within the first intron of C9ORF72 constitutes the most common cause of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD). Through repeat-associated non-ATG translation, these expansions are translated into dipeptide… read more here.
Keywords: bet bromodomain; toxicity; chemical screen; c9orf72 ... See more keywords
Alternative Mechanisms for DNA Engagement by BET Bromodomain-Containing Proteins.
Sign Up to like & getrecommendations! Published in 2022 at "Biochemistry"
DOI: 10.1021/acs.biochem.2c00157
Abstract: Epigenetic reader domains regulate chromatin structure and modulate gene expression through the recognition of post-translational modifications on histones. Recently, reader domains have also been found to harbor double-stranded (ds) DNA-binding activity, which is as functionally… read more here.
Keywords: dna engagement; bet; mechanisms dna; bet bromodomain ... See more keywords
BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.6b01336
Abstract: Chemical inhibition of epigenetic regulatory proteins BrdT and Brd4 is emerging as a promising therapeutic strategy in contraception, cancer, and heart disease. We report an easily synthesized dihydropyridopyrimidine pan-BET inhibitor scaffold, which was uncovered via… read more here.
Keywords: bet bromodomain; virtual screen; screen; bromodomain inhibitors ... See more keywords
Combined BET bromodomain and CDK2 inhibition in MYC-driven medulloblastoma
Sign Up to like & getrecommendations! Published in 2018 at "Oncogene"
DOI: 10.1038/s41388-018-0135-1
Abstract: Medulloblastoma (MB) is the most common malignant brain tumor in children. MYC genes are frequently amplified and correlate with poor prognosis in MB. BET bromodomains recognize acetylated lysine residues and often promote and maintain MYC… read more here.
Keywords: bet bromodomain; medulloblastoma; inhibition; myc driven ... See more keywords
Enhancer Domains in Gastrointestinal Stromal Tumor Regulate KIT Expression and Are Targetable by BET Bromodomain Inhibition.
Sign Up to like & getrecommendations! Published in 2019 at "Cancer research"
DOI: 10.1158/0008-5472.can-18-1888
Abstract: Gastrointestinal stromal tumor (GIST) is a mesenchymal neoplasm characterized by activating mutations in the related receptor tyrosine kinases KIT and PDGFRA. GIST relies on expression of these unamplified receptor tyrosine kinase (RTK) genes through a… read more here.
Keywords: expression; bet bromodomain; kinase; enhancer ... See more keywords
Abstract 5069: Inhibition of BET bromodomain, epigenetic regulator, as an effective therapeutic approach for gastric cancer
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-5069
Abstract: Epigenetic dysregulation is a common characteristic of cancer, including gastric cancer(GC), which ultimately contributes to the development and progression of GC. Sequencing of cancer genomes has revealed frequent mutations in epigenetic regulators, particularly chromatin remodelers… read more here.
Keywords: inhibition bet; bet bromodomain; gastric cancer; epigenetic regulator ... See more keywords
Abstract B34: Novel synergistic combination therapies with BET bromodomain inhibitors in triple-negative breast cancer
Sign Up to like & getrecommendations! Published in 2018 at "Molecular Cancer Research"
DOI: 10.1158/1557-3125.advbc17-b34
Abstract: Adaptive resistance to targeted cancer therapies is a universal problem in cancer treatment where tumor cells circumvent targeted pathway inhibition to reactivate growth signaling. In our previous work, we observed genome-wide enhancer remodeling following MEK… read more here.
Keywords: negative breast; bet bromodomain; inhibition; breast cancer ... See more keywords
BET bromodomain proteins regulate transcriptional reprogramming in genetic dilated cardiomyopathy.
Sign Up to like & getrecommendations! Published in 2020 at "JCI insight"
DOI: 10.1172/jci.insight.138687
Abstract: The bromodomain and extraterminal (BET) family of epigenetic reader proteins are key regulators of inflammatory and hypertrophic gene expression in the heart. We previously identified the activation of pro-inflammatory gene networks as a key early… read more here.
Keywords: bet bromodomain; inflammatory gene; bet; gene ... See more keywords
BET-bromodomain and EZH2 inhibitor treated chronic GVHD mice have blunted germinal centers with distinct transcriptomes.
Sign Up to like & getrecommendations! Published in 2022 at "Blood"
DOI: 10.1182/blood.2021014557
Abstract: Despite advances in the field, chronic graft-vs-host-disease (cGVHD) remains a leading cause of morbidity and mortality following allogenic hematopoietic stem cell transplant. As treatment options remain limited, we tested efficacy of anti-cancer, chromatin modifying enzyme… read more here.
Keywords: ezh2 inhibitor; jq5; bet bromodomain; inhibitor ... See more keywords
Immunogenicity of prostate cancer is augmented by BET bromodomain inhibition
Sign Up to like & getrecommendations! Published in 2019 at "Journal for Immunotherapy of Cancer"
DOI: 10.1186/s40425-019-0758-y
Abstract: BackgroundProstate cancer responds poorly to current immunotherapies. Epigenetic therapies such as BET Bromodomain inhibition can change the transcriptome of tumor cells, possibly making them more immunogenic and thus susceptible to immune targeting.MethodsWe characterized the effects… read more here.
Keywords: prostate cancer; bromodomain inhibition; inhibition; bet bromodomain ... See more keywords
N-terminal BET bromodomain inhibitors disrupt a BRD4-p65 interaction and reduce inducible nitric oxide synthase transcription in pancreatic β-cells
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Endocrinology"
DOI: 10.3389/fendo.2022.923925
Abstract: Chronic inflammation of pancreatic islets is a key driver of β-cell damage that can lead to autoreactivity and the eventual onset of autoimmune diabetes (T1D). In the islet, elevated levels of proinflammatory cytokines induce the… read more here.
Keywords: interaction; inhibition; bet; transcription ... See more keywords