Selective inhibition of BET bromodomains

Filippakopoulos, Panagis, Qi, Jun, Picaud, Sarah, Shen, Yao, Smith, William B., Fedorov, Oleg, Morse, Elizabeth M., Keates, Tracey, Hickman, Tyler T., Felletar, Ildiko, Philpott, Martin, Munro, Shonagh, McKeown, Michael R., Wang, Yuchuan, Christie, Amanda L., West, Nathan, Cameron, Michael J., Schwartz, Brian, Heightman, Tom D., La Thangue, Nicholas, French, Christopher A., Wiest, Olaf, Kung, Andrew L., Knapp, Stefan, Bradner, James E.·2010·Nature

DOI 10.1038/nature09504

Cited by (1,029)

Items 101–200 of 1,029

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Target validation using chemical probes
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Brd4 and JMJD6-Associated Anti-Pause Enhancers in Regulation of Transcriptional Pause Release
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BRD4 Connects Enhancer Remodeling to Senescence Immune Surveillance
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Combined inhibition of BET family proteins and histone deacetylases as a potential epigenetics-based therapy for pancreatic ductal adenocarcinoma
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BET Bromodomains Mediate Transcriptional Pause Release in Heart Failure
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The bromodomain interaction module
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AF9 YEATS Domain Links Histone Acetylation to DOT1L-Mediated H3K79 Methylation
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Inderpreet Sur, Jussi Taipale · 2016 · Nature reviews. Cancer
Clinical Response of Carcinomas Harboring the BRD4–NUT Oncoprotein to the Targeted Bromodomain Inhibitor OTX015/MK-8628
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BET inhibitors: a novel epigenetic approach
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BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia
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Light-Induced Protein Degradation with Photocaged PROTACs
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Dawson, Mark A. · 2017 · Science
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Bing Nan Zhou, Jiantao Hu, Fuming Xu, Zhuo Chen, Longchuan Bai, Ester Fernández‐Salas, Mei Lin, Liu Liu, Chao‐Yie Yang, Yujun Zhao et al. · 2017 · Journal of Medicinal Chemistry
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Birgit Knoechel, Justine E. Roderick, Kaylyn E. Williamson, Jiang Zhu, Jens G. Lohr, Matthew J. Cotton, Shawn M. Gillespie, Daniel E. Fernandez, Manching Ku, Hongfang Wang et al. · 2014 · Nature Genetics
Lysine Acetylation Goes Global: From Epigenetics to Metabolism and Therapeutics
Ibraheem Ali, Ryan J. Conrad, Eric M. Verdin, Mélanie Ott · 2018 · Chemical Reviews
SLAM-seq defines direct gene-regulatory functions of the BRD4-MYC axis
Matthias Muhar, Anja Ebert, Tobias Neumann, Christian Umkehrer, Julian Jude, Corinna Wieshofer, Philipp Rescheneder, Jesse Lipp, Veronika A. Herzog, Brian Reichholf et al. · 2018 · Science
Cardiac fibrosis: Myofibroblast-mediated pathological regulation and drug delivery strategies
Mengrui Liu, Blanca López de Juan Abad, Ke Cheng · 2021 · Advanced Drug Delivery Reviews
Achieving clinical success with BET inhibitors as anti-cancer agents
Tatiana Shorstova, William D. Foulkes, Michael Witcher · 2021 · British Journal of Cancer
The emerging role of mass spectrometry-based proteomics in drug discovery
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Oxidants, antioxidants and the current incurability of metastatic cancers
Jim Watson · 2013 · Open Biology
ecDNA hubs drive cooperative intermolecular oncogene expression
King L. Hung, Kathryn E. Yost, Liangqi Xie, Quanming Shi, Konstantin Helmsauer, Jens Luebeck, Robert Schöpflin, Joshua T. Lange, Rocío Chamorro González, Natasha E. Weiser et al. · 2021 · Nature
Super-Enhancer-Driven Transcriptional Dependencies in Cancer
Satyaki Sengupta, Rani E. George · 2017 · Trends in cancer
HIV-1 transcription and latency: an update
Carine M. Van Lint, Sophie Bouchat, Alessandro Marcello · 2013 · Retrovirology
The Ubiquitin Ligase FBXW7 Modulates Leukemia-Initiating Cell Activity by Regulating MYC Stability
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Prostate cancer–associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4
Xiangpeng Dai, Wenjian Gan, Xiaoning Li, Shangqian Wang, Wei Zhang, Ling Huang, Shengwu Liu, Qing Zhong, Jianping Guo, Jinfang Zhang et al. · 2017 · Nature Medicine
MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53
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Y. Taniguchi · 2016 · International Journal of Molecular Sciences
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MYC protein interactors in gene transcription and cancer
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Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins
Lockwood, William W., Zejnullahu, Kreshnik, Bradner, James E., Varmus, Harold · 2012 · Proceedings of the National Academy of Sciences
BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia
Jae‐Seok Roe, Fatih Mercan, Keith D. Rivera, Darryl Pappin, Christopher R. Vakoc · 2015 · Molecular Cell
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Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains
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