Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c00566
Abstract: The bromodomain and extraterminal domain (BET) family of epigenetic regulators comprises four proteins (BRD2, BRD3, BRD4, BRDT), each containing tandem bromodomains. To date, small molecule inhibitors of these proteins typically bind all eight bromodomains of… read more here.
Keywords: anti inflammatory; extraterminal domain; inflammatory antiproliferative; domain bet ... See more keywords
Bromodomain and extraterminal protein-targeted probe enables tumour visualisation in vivo using positron emission tomography.
Sign Up to like & getrecommendations! Published in 2023 at "Chemical communications"
DOI: 10.1039/d2cc04813b
Abstract: Bromodomain and extraterminal (BET) proteins, a family of epigenetic regulators, have emerged as important oncology drug targets. BET proteins have not been targeted for molecular imaging of cancer. Here, we report the development of a… read more here.
Keywords: targeted probe; bromodomain extraterminal; enables tumour; probe enables ... See more keywords
Trotabresib, an oral potent bromodomain and extraterminal inhibitor, in patients with high-grade gliomas: A phase I, “window-of-opportunity” study
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DOI: 10.1093/neuonc/noac263
Abstract: Abstract Background The bromodomain and extraterminal protein (BET) inhibitor trotabresib has demonstrated antitumor activity in patients with advanced solid tumors, including high-grade gliomas. CC-90010-GBM-001 (NCT04047303) is a phase I study investigating the pharmacokinetics, pharmacodynamics, and… read more here.
Keywords: high grade; grade gliomas; trotabresib; bromodomain extraterminal ... See more keywords
Targeting basal-like breast tumors with bromodomain and extraterminal domain (BET) and polo-like kinase inhibitors
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DOI: 10.18632/oncotarget.14465
Abstract: Metastatic triple negative breast cancer (TNBC) is an incurable disease with limited therapeutic options, and no targeted therapies available. Triple negative tumors and the basal-like genomic subtype, are both characterized by a high proliferation rate… read more here.
Keywords: basal like; extraterminal domain; kinase; cell division ... See more keywords
Bromodomain and Extraterminal Protein Inhibitor, Apabetalone (RVX-208), Reduces ACE2 Expression and Attenuates SARS-Cov-2 Infection In Vitro
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DOI: 10.3390/biomedicines9040437
Abstract: Effective therapeutics are urgently needed to counter infection and improve outcomes for patients suffering from COVID-19 and to combat this pandemic. Manipulation of epigenetic machinery to influence viral infectivity of host cells is a relatively… read more here.
Keywords: infection; infection vitro; sars cov; cov infection ... See more keywords