Results 1 to 10 of about 56,924 (160)

A Minireview on BET Inhibitors: Beyond Bromodomain Targeting [PDF]

Biomedicines
Bromodomain and extra-terminal domain (BET) proteins are epigenetic readers that recognize the histone acetylation code and play a critical role in regulating gene transcription.
Mikhail S. Iudin, Yuri M. Khodarovich, Anna M. Varizhuk, Vladimir B. Tsvetkov, Vyacheslav V. Severov   +4 more
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The emerging role of BET inhibitors in breast cancer [PDF]

Breast, 2020
Bromodomain and extraterminal domain (BET) proteins are epigenetic molecules that regulate the expression of multiple genes involved in carcinogenesis.
Angeliki Andrikopoulou, Michalis Liontos, Konstantinos Koutsoukos, Meletios-Athanasios Dimopoulos, Flora Zagouri   +4 more
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Identification of BET inhibitors (BETi) against solitary fibrous tumor (SFT) through high-throughput screening (HTS) [PDF]

Neoplasia: An International Journal for Oncology Research
Cancers, especially fusion oncoprotein (FO)-driven hematological cancers and sarcomas, often develop from a low number of key mutations. Solitary Fibrous Tumor (SFT) is a rare mesenchymal tumor driven by the NAB2-STAT6 oncofusion gene.
Jose L. Mondaza-Hernandez, David S. Moura, Yi Li, Jesus L. Marti, Paulino Gomez-Puertas, John T. Nguyen, Shuguang Wei, Bruce A. Posner, Clark A. Meyer, Leonidas Bleris, Javier Martin-Broto, Heather N. Hayenga   +11 more
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RAPID resistance to BET inhibitors is mediated by FGFR1 in glioblastoma [PDF]

Scientific Reports
Bromodomain and extra-terminal domain (BET) proteins are therapeutic targets in several cancers including the most common malignant adult brain tumor glioblastoma (GBM). Multiple small molecule inhibitors of BET proteins have been utilized in preclinical
Anna M. Jermakowicz, Alison M. Kurimchak, Katherine J. Johnson, Florence Bourgain-Guglielmetti, Simon Kaeppeli, Maurizio Affer, Hari Pradhyumnan, Robert K. Suter, Winston Walters, Maria Cepero, James S. Duncan, Nagi G. Ayad   +11 more
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Pharmacologic screen identifies active combinations with BET inhibitors and LRRK2 as a novel putative target in lymphoma [PDF]

eJHaem, 2022
Inhibitors of the Bromo‐ and Extra‐Terminal domain (BET) family proteins have strong preclinical antitumor activity in multiple tumor models, including lymphomas. Limited single‐agent activity has been reported in the clinical setting.
Filippo Spriano, Giulio Sartori, Chiara Tarantelli, Marilia Barreca, Gaetanina Golino, Andrea Rinaldi, Sara Napoli, Michele Mascia, Lorenzo Scalise, Alberto J. Arribas, Luciano Cascione, Emanuele Zucca, Anastasios Stathis, Eugenio Gaudio, Francesco Bertoni   +14 more
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Safety and Efficacy of Bromodomain and Extra-Terminal Inhibitors for the Treatment of Hematological Malignancies and Solid Tumors: A Systematic Study of Clinical Trials

Frontiers in Pharmacology, 2021
Background: The upregulated expression of BET proteins is closely associated with the occurrence and development of hematological malignancies and solid tumors.
Yanli Sun, Yanli Sun, Jie Han, Zhanzhao Wang, Xuening Li, Yanhua Sun, Zhenbo Hu, Zhenbo Hu   +7 more
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BET Bromodomain Inhibitors: Novel Design Strategies and Therapeutic Applications

Molecules, 2023
The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer-related and immunity-associated genes.
Kenneth K. W. To, Enming Xing, Ross C. Larue, Pui-Kai Li   +3 more
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Bromodomain and extraterminal (BET) proteins: biological functions, diseases and targeted therapy

Signal Transduction and Targeted Therapy, 2023
BET proteins, which influence gene expression and contribute to the development of cancer, are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic anticancer treatment.
Zhi-Qiang Wang, Zhao-Cong Zhang, Yu-Yang Wu, Ya-Nan Pi, Sheng-Han Lou, Tian-Bo Liu, Ge Lou, Chang Yang   +7 more
doaj   +1 more source

BET bromodomain inhibitor HMBA synergizes with MEK inhibition in treatment of malignant glioma

Epigenetics, 2021
(1) Background: BET bromodomain proteins regulate transcription by binding acetylated histones and attracting key factors for, e.g., transcriptional elongation.
Elisa Funck-Brentano, Dzeneta Vizlin-Hodzic, Jonas A. Nilsson, Lisa M. Nilsson   +3 more
doaj   +1 more source

Targeting CBX3 with a Dual BET/PLK1 Inhibitor Enhances the Antitumor Efficacy of CDK4/6 Inhibitors in Prostate Cancer

Advanced Science, 2023
The development of castration‐resistant prostate cancer (CRPC) is a significant factor that reduces life expectancy among patients with prostate cancer.
Huaiyuan Liang, Chunguang Yang, Ruijiang Zeng, Yingqiu Song, Jianxi Wang, Wei Xiong, Binyuan Yan, Xin Jin   +7 more
doaj   +1 more source