Rational design and development of selective BRD7 bromodomain inhibitors and their activity in prostate cancer (original) (raw)
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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Diving into the water: Inducible binding conformations for BRD4, TAF1(2), BRD9, and CECR2 bromodomains
James Audia
Journal of medicinal chemistry, 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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Potent and Selective N-Terminal BRD4 Bromodomain Inhibitors by Targeting Non-Conserved Residues and Structured Water Displacement
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LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor
Lucas Vieira
Angewandte Chemie, 2015
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Structural variation of protein-ligand complexes of the first bromodomain of BRD4
Stephen Pickett
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IDENTIFICATION OF POTENT BROMODOMAIN4 (BRD4) INHIBITORS BY ENERGY-PHARMACOPHORE BASED VIRTUAL SCREENING TO TARGET BRD4-NUT MIDLINE CARCINOMA
International Journal of Pharmacy and Pharmaceutical Sciences (IJPPS)
International Journal of Pharmacy and Pharmaceutical Sciences, 2015
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Preparation data of the bromodomains BRD3(1), BRD3(2), BRD4(1), and BRPF1B and crystallization of BRD4(1)-inhibitor complexes
Xavier Lucas, Stefan Gerhardt
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In Silico Design and Molecular Basis for the Selectivity of Olinone Towards the First over the Second Bromodomain of BRD4
Yoel Betancourt
Proteins: Structure, Function, and Bioinformatics, 2019
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Identification of a novel ligand for the ATAD2 bromodomain with selectivity over BRD4 through a fragment growing approach
santosh adhikari
Organic & biomolecular chemistry, 2018
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Pyronaridine as a Bromodomain-Containing Protein 4-N-Terminal Bromodomain (BRD4-BD1) Inhibitor: In Silico Database Mining, Molecular Docking, and Molecular Dynamics Simulation
Alaa Abdelrahman
Molecules, 2023
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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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Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor
Jannik Andersen
Journal of Medicinal Chemistry, 2015
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The bromodomain: from epigenome reader to druggable target
Roberto Sanchez
Biochimica et biophysica acta, 2014
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Chemical Proteomic Profiling of Bromodomains Enables the Wide-Spectrum Evaluation of Bromodomain Inhibitors in Living Cells
xiucong bao
Journal of the American Chemical Society, 2019
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4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1)
Xavier Lucas, Stefan Gerhardt
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Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit
Gerwyn Bish, Sarah Picaud, Nunzio Sciammetta
Journal of Medicinal Chemistry, 2012
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Controlling Intramolecular Interactions in the Design of Selective, High-Affinity, Ligands for the CREBBP Bromodomain
Kirsten Christensen
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An Activity-Based Probe Targeting Non-Catalytic, Highly Conserved Amino Acid Residues within Bromodomains
Kathryn Pugh
Angewandte Chemie International Edition
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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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Selective inhibition of BET bromodomains
Amanda Christie
2010
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A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes
shalil khanal
Journal of Medicinal Chemistry, 2022
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Identification of a Novel Class of BRD4 Inhibitors by Computational Screening and Binding Simulations
Ernst Schonbrunn
ACS Omega
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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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Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability
Alessandra Pasquo
PLOS ONE, 2016
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Potent and selective bivalent inhibitors of BET bromodomains
Michael Waring
Nature Chemical Biology, 2016
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Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains
Ting-Chao Chou
ACS Chemical Biology, 2013
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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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9 H -Purine Scaffold Reveals Induced-Fit Pocket Plasticity of the BRD9 Bromodomain
Gianluigi Lauro
Journal of Medicinal Chemistry, 2015
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Biased multicomponent reactions to develop novel bromodomain inhibitors
Asha kadam
Journal of medicinal chemistry, 2014
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BET Bromodomain Inhibitors With One-step Synthesis Discovered from Virtual Screen
Norbert Berndt
Journal of medicinal chemistry, 2017
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Structure and acetyl-lysine recognition of the bromodomain
Shiraz Mujtaba
Oncogene, 2007
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Structure-based design of highly selective inhibitors of the CREB binding protein bromodomain
Jotham Coe
Journal of medicinal chemistry, 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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