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Times Cited: 55
Times Cited: 55
Times Cited
Times Co-cited
Similarity
Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer.
Emily J Faivre, Keith F McDaniel, Daniel H Albert, Srinivasa R Mantena, Joshua P Plotnik, Denise Wilcox, Lu Zhang, Mai H Bui, George S Sheppard, Le Wang,[...]. Nature 2020
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Selective inhibition of BET bromodomains.
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Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation.
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Omer Gilan, Inmaculada Rioja, Kathy Knezevic, Matthew J Bell, Miriam M Yeung, Nicola R Harker, Enid Y N Lam, Chun-Wa Chung, Paul Bamborough, Massimo Petretich,[...]. Science 2020
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Histone recognition and large-scale structural analysis of the human bromodomain family.
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Targeting bromodomains: epigenetic readers of lysine acetylation.
Panagis Filippakopoulos, Stefan Knapp. Nat Rev Drug Discov 2014
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The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.
Jonathan T Seal, Stephen J Atkinson, Helen Aylott, Paul Bamborough, Chun-Wa Chung, Royston C B Copley, Laurie Gordon, Paola Grandi, James R J Gray, Lee A Harrison,[...]. J Med Chem 2020
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RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
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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.
Christopher R Wellaway, Paul Bamborough, Sharon G Bernard, Chun-Wa Chung, Peter D Craggs, Leanne Cutler, Emmanuel H Demont, John P Evans, Laurie Gordon, Bhumika Karamshi,[...]. J Med Chem 2020
Christopher R Wellaway, Paul Bamborough, Sharon G Bernard, Chun-Wa Chung, Peter D Craggs, Leanne Cutler, Emmanuel H Demont, John P Evans, Laurie Gordon, Bhumika Karamshi,[...]. J Med Chem 2020
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Drug Discovery Targeting Bromodomain-Containing Protein 4.
Zhiqing Liu, Pingyuan Wang, Haiying Chen, Eric A Wold, Bing Tian, Allan R Brasier, Jia Zhou. J Med Chem 2017
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Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins.
Alex Preston, Stephen Atkinson, Paul Bamborough, Chun-Wa Chung, Peter D Craggs, Laurie Gordon, Paola Grandi, James R J Gray, Emma J Jones, Matthew Lindon,[...]. J Med Chem 2020
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Suppression of inflammation by a synthetic histone mimic.
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GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.
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Bromodomains: a new target class for drug development.
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Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
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RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia.
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GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.
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Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
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BET bromodomain inhibition as a therapeutic strategy to target c-Myc.
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BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses.
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AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies.
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Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.
Brian K Albrecht, Victor S Gehling, Michael C Hewitt, Rishi G Vaswani, Alexandre Côté, Yves Leblanc, Christopher G Nasveschuk, Steve Bellon, Louise Bergeron, Robert Campbell,[...]. J Med Chem 2016
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Structure and ligand of a histone acetyltransferase bromodomain.
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First-in-human phase I study of the bromodomain and extraterminal motif inhibitor BAY 1238097: emerging pharmacokinetic/pharmacodynamic relationship and early termination due to unexpected toxicity.
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Clinical trials for BET inhibitors run ahead of the science.
Guillaume Andrieu, Anna C Belkina, Gerald V Denis. Drug Discov Today Technol 2016
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Selective chemical modulation of gene transcription favors oligodendrocyte lineage progression.
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Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
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20
RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.
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Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
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Discovery of Benzo[cd]indol-2(1H)-ones and Pyrrolo[4,3,2-de]quinolin-2(1H)-ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain with Potential High Efficiency against Acute Gouty Arthritis.
Fei Jiang, Qinghua Hu, Zhimin Zhang, Hongmei Li, Huili Li, Dewei Zhang, Hanwen Li, Yu Ma, Jingjing Xu, Haifang Chen,[...]. J Med Chem 2019
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Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.
Olivier Mirguet, Romain Gosmini, Jérôme Toum, Catherine A Clément, Mélanie Barnathan, Jean-Marie Brusq, Jacqueline E Mordaunt, Richard M Grimes, Miriam Crowe, Olivier Pineau,[...]. J Med Chem 2013
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Bromodomain inhibitor OTX015 in patients with lymphoma or multiple myeloma: a dose-escalation, open-label, pharmacokinetic, phase 1 study.
Sandy Amorim, Anastasios Stathis, Mary Gleeson, Sunil Iyengar, Valeria Magarotto, Xavier Leleu, Franck Morschhauser, Lionel Karlin, Florence Broussais, Keyvan Rezai,[...]. Lancet Haematol 2016
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Epigenetic drug discovery: breaking through the immune barrier.
David F Tough, Paul P Tak, Alexander Tarakhovsky, Rab K Prinjha. Nat Rev Drug Discov 2016
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Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762.
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Discovery and characterization of small molecule inhibitors of the BET family bromodomains.
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The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs.
Michela Boi, Eugenio Gaudio, Paola Bonetti, Ivo Kwee, Elena Bernasconi, Chiara Tarantelli, Andrea Rinaldi, Monica Testoni, Luciano Cascione, Maurilio Ponzoni,[...]. Clin Cancer Res 2015
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RVX-297- a novel BD2 selective inhibitor of BET bromodomains.
Olesya A Kharenko, Emily M Gesner, Reena G Patel, Karen Norek, Andre White, Eric Fontano, Robert K Suto, Peter R Young, Kevin G McLure, Henrik C Hansen. Biochem Biophys Res Commun 2016
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RVX-297, a BET Bromodomain Inhibitor, Has Therapeutic Effects in Preclinical Models of Acute Inflammation and Autoimmune Disease.
Ravi Jahagirdar, Sarah Attwell, Suzana Marusic, Alison Bendele, Narmada Shenoy, Kevin G McLure, Dean Gilham, Karen Norek, Henrik C Hansen, Raymond Yu,[...]. Mol Pharmacol 2017
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Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins.
Deheng Chen, Tian Lu, Ziqin Yan, Wenchao Lu, Feilong Zhou, Xilin Lyu, Biling Xu, Hualiang Jiang, Kaixian Chen, Cheng Luo,[...]. Eur J Med Chem 2019
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BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice.
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Structural basis of PROTAC cooperative recognition for selective protein degradation.
Morgan S Gadd, Andrea Testa, Xavier Lucas, Kwok-Ho Chan, Wenzhang Chen, Douglas J Lamont, Michael Zengerle, Alessio Ciulli. Nat Chem Biol 2017
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Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).
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BRD4 and Cancer: going beyond transcriptional regulation.
Benedetta Donati, Eugenia Lorenzini, Alessia Ciarrocchi. Mol Cancer 2018
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BET domain co-regulators in obesity, inflammation and cancer.
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The mechanisms behind the therapeutic activity of BET bromodomain inhibition.
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Targeting Brd4 for cancer therapy: inhibitors and degraders.
Yingchao Duan, Yuanyuan Guan, Wenping Qin, Xiaoyu Zhai, Bin Yu, Hongmin Liu. Medchemcomm 2018
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DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation.
Georg E Winter, Dennis L Buckley, Joshiawa Paulk, Justin M Roberts, Amanda Souza, Sirano Dhe-Paganon, James E Bradner. Science 2015
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Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
Zhiqing Liu, Haiying Chen, Pingyuan Wang, Yi Li, Eric A Wold, Paul G Leonard, Sarah Joseph, Allan R Brasier, Bing Tian, Jia Zhou. J Med Chem 2020
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First-in-Human Study of Mivebresib (ABBV-075), an Oral Pan-Inhibitor of Bromodomain and Extra Terminal Proteins, in Patients with Relapsed/Refractory Solid Tumors.
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Co-cited is the co-citation frequency, indicating how many articles cite the article together with the query article. Similarity is the co-citation as percentage of the times cited of the query article or the article in the search results, whichever is the lowest. These numbers are calculated for the last 100 citations when articles are cited more than 100 times.