Design and characterization of bivalent BET inhibitors (original) (raw)
AZD5153: a novel bivalent BET bromodomain inhibitor highly active against hematologic malignancies
Michael Waring
Molecular cancer therapeutics, 2016
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Selective inhibition of BET bromodomains
Amanda Christie
2010
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Potent and selective bivalent inhibitors of BET bromodomains
Michael Waring
Nature Chemical Biology, 2016
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Bromodomain and extraterminal domain inhibitors (BETi) for cancer therapy: chemical modulation of chromatin structure
Inam Khan
Cold Spring Harbor perspectives in biology, 2014
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Bromodomain and extra-terminal motif inhibitors: a review of preclinical and clinical advances in cancer therapy
Talal KHAN
Future Science OA, 2019
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Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia
Mai Bùi
Molecular Cancer Therapeutics, 2021
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Pharmacological Targeting of BET Bromodomain Proteins in Acute Myeloid Leukemia and Malignant Lymphomas: From Molecular Characterization to Clinical Applications
Gael Roue
Cancers, 2019
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Targeting MYC dependence in cancer by inhibiting BET bromodomains
Pria Sandy
2011
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Targeting the BET family for the treatment of leukemia
Xavier Lucas
Epigenomics, 2014
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A chemical toolbox for the study of bromodomains and epigenetic signaling
Jeffrey Dilworth
Nature Communications, 2019
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The bromodomain: from epigenome reader to druggable target
Roberto Sanchez
Biochimica et biophysica acta, 2014
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Bromodomains as therapeutic targets in cancer
isaia barbieri
Briefings in functional genomics, 2013
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Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase–Bromodomain Inhibitor
Huarui Cui
Journal of Medicinal Chemistry
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Bromodomain-Selective BET Inhibitors Are Potent Antitumor Agents against MYC-Driven Pediatric Cancer
Anang Shelat
Cancer Research, 2020
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Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability
Alessandra Pasquo
PLOS ONE, 2016
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Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer
Yuchen Bai
Oncotarget, 2013
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A bromodomain-DNA interaction facilitates acetylation-dependent bivalent nucleosome recognition by the BET protein BRDT
Christoph Müller
2016
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The Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition
Anne-Marie Michon
Journal of medicinal chemistry, 2015
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Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains
Guangtao Zhang
Journal of Medicinal Chemistry, 2013
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The BET Bromodomain inhibitor OTX015 affects pathogenetic pathways in pre-clinical B-cell tumor models and synergizes with targeted drugs
Esteban Cvitkovic
Clinical Cancer Research, 2015
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Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery
Trang Tieu
Epigenetics & chromatin, 2015
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Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain
Mai Bùi
Journal of Medicinal Chemistry, 2020
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Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A)
David Lugo
Bioorganic & medicinal chemistry letters, 2012
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Discovery and characterization of bromodomain 2–specific inhibitors of BRDT
Sureshbabu Nagarajan
Proceedings of the National Academy of Sciences, 2021
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The Making of I-BET762, a BET Bromodomain Inhibitor Now in Clinical Development
Chao-yie Yang
Journal of Medicinal Chemistry, 2013
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Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors
Ernst Schonbrunn
ACS Chemical Biology, 2014
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BET bromodomain proteins are required for glioblastoma cell proliferation
regina graham
Epigenetics, 2014
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Preclinical characterization of BET family bromodomain inhibitor ABBV-075 suggests combination therapeutic strategies
Mai Bùi
Cancer research, 2017
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Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies
Anne Cheasty
Journal of medicinal chemistry, 2017
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Observed bromodomain flexibility reveals histone peptide- and small molecule ligand-compatible forms of ATAD2A
Jannik Andersen
Biochemical Journal, 2014
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Molecular Insights into the Recognition of N-Terminal Histone Modifications by the BRPF1 Bromodomain
Stefan Balaz
Journal of Molecular Biology, 2014
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