Results 1 to 10 of about 24,956 (275)

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
doaj   +10 more sources

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
doaj   +7 more sources

RAPID resistance to BET inhibitors is mediated by FGFR1 in glioblastoma [PDF]

Scientific Reports, 2023
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
doaj   +5 more sources

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
doaj   +4 more sources

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   +2 more sources

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
doaj   +2 more sources

BET Inhibitors Synergize with Carfilzomib to Induce Cell Death in Cancer Cells via Impairing Nrf1 Transcriptional Activity and Exacerbating the Unfolded Protein Response

Biomolecules, 2020
Currently, proteasome inhibitors bortezomib, carfilzomib, and ixazomib are successfully used in clinics to treat multiple myeloma. However, these agents show limited efficacy against solid tumors. Identification of drugs that can potentiate the action of
Janakiram R. Vangala, Ajay Potluri, Senthil K. Radhakrishnan   +2 more
doaj   +3 more sources

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
doaj   +2 more sources

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
doaj   +1 more source

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