The novel BET inhibitor UM-002 reduces glioblastoma cell proliferation and invasion [PDF]
Scientific Reports, 2021 Bromodomain and extraterminal domain (BET) proteins have emerged as therapeutic targets in multiple cancers, including the most common primary adult brain tumor glioblastoma (GBM).
Anna M. Jermakowicz +6 more
doaj +3 more sources
Apabetalone, a Clinical-Stage, Selective BET Inhibitor, Opposes DUX4 Target Gene Expression in Primary Human FSHD Muscle Cells [PDF]
Biomedicines, 2023 Facioscapulohumeral dystrophy (FSHD) is a muscle disease caused by inappropriate expression of the double homeobox 4 (DUX4) gene in skeletal muscle, and its downstream activation of pro-apoptotic transcriptional programs.
Christopher D. Sarsons +9 more
doaj +2 more sources
Sustained Clinical Response to Immunotherapy Followed by BET Inhibitor in a Patient with Unresectable Sinonasal NUT Carcinoma [PDF]
Journal of Immunotherapy and Precision OncologyNUT carcinomas (NCs) are a group of rare tumors that can occur anywhere in the body and are defined by the fusion of the nuclear protein in testis (NUTM1) resulting in increased transcription of proto-oncogenes.
Harriet Herbison +4 more
doaj +2 more sources
Comprehensive transcriptome profiling of BET inhibitor-treated HepG2 cells. [PDF]
PLoS ONE, 2022 Hepatocellular carcinoma (HCC) is the most common primary liver cancer and poor prognosis. Emerging evidence suggests that epigenetic alterations play a crucial role in HCC, suggesting epigenetic inhibition as a promising therapeutic approach.
Mina Baek +7 more
doaj +2 more sources
BET inhibitor trotabresib in heavily pretreated patients with solid tumors and diffuse large B-cell lymphomas [PDF]
Nature Communications, 2023 Bromodomain and extraterminal proteins (BET) are reported as targets for anticancer therapy. Here, the authors report the final results of a phase I clinical trial of the BET inhibitor trotabresib in patients with solid tumours and diffuse large B-cell ...
Victor Moreno +20 more
doaj +2 more sources
Modulation of Virulence-Associated Traits in Aspergillus fumigatus by BET Inhibitor JQ1 [PDF]
Microorganisms, 2022 Aspergillus fumigatus is a disease-causing, opportunistic fungus that can establish infection due to its capacity to respond to a wide range of environmental conditions.
Anastasia Orekhova +12 more
doaj +2 more sources
The BET inhibitor JQ1 targets fat metabolism and counteracts obesity [PDF]
Journal of Advanced ResearchIntroduction: Obesity, one of the most frequent health problems in the adult population, is a condition characterized by excessive white adipose tissue accumulation and accompanied by the increased risk to develop other disorders such as type II diabetes,
Claudia Fornelli +7 more
doaj +2 more sources
Retinoblastoma protein as an intrinsic BRD4 inhibitor modulates small molecule BET inhibitor sensitivity in cancer [PDF]
Nature Communications, 2022 Here the authors identify retinoblastoma (RB) protein as an intrinsic inhibitor of BRD4 and demonstrate that loss of RB induces BRD4 cistrome changes in the genome and enrichment of GPCR-cAMP signaling pathway, conferring resistance to small molecule BET
Donglin Ding +8 more
doaj +2 more sources
Epigenetic therapy: BBC1115, a novel BET inhibitor with broad antitumor activity [PDF]
Molecular Therapy: Nucleic Acids, 2023 Pradeep Reddy Cingaram
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Exploration of Targeted Anti-tumor Therapy, 2021 Aim: Bromodomain and extra-terminal domain (BET) proteins are epigenetic readers that play a fundamental role in transcription regulation. Preclinical and early clinical evidence sustain BET targeting as an anti-cancer approach.
Chiara Tarantelli +14 more
doaj +1 more source