Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands - Test2 - elhamkhani - TriplyDB

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

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The bromodomain: from epigenome reader to druggable target Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors Observed bromodomain flexibility reveals histone peptide- and small molecule ligand-compatible forms of ATAD2 Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors Targeting bromodomains: epigenetic readers of lysine acetylation Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains Drug Discovery Targeting Bromodomain-Containing Protein 4.Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains BET bromodomain inhibitors: a patent review.[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains Biased multicomponent reactions to develop novel bromodomain inhibitors.Small-molecule modulators for epigenetics targets.Preparation of small-molecule microarrays by trans-cyclooctene tetrazine ligation and their application in the high-throughput screening of protein-protein interaction inhibitors of bromodomains.Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain.The photochemical thiol-ene reaction as a versatile method for the synthesis of glutathione S-conjugates targeting the bacterial potassium efflux system Kef.BET inhibition as a new strategy for the treatment of gastric cancer.Accurate calculation of the absolute free energy of binding for drug molecules.Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.Erythropoiesis provides a BRD's eye view of BET protein function.Phenotypic screening and fragment-based approaches to the discovery of small-molecule bromodomain ligands.Bromodomains and their pharmacological inhibitors.Emerging therapeutic targets in human acute myeloid leukemia (part 2) - bromodomain inhibition should be considered as a possible strategy for various patient subsets.The oxygenase Jmjd6--a case study in conflicting assignments.Fragment-Based Drug Discovery in the Bromodomain and Extra-Terminal Domain Family.Progress in the Development of non-BET Bromodomain Chemical Probes.Bromodomains in Protozoan Parasites: Evolution, Function, and Opportunities for Drug Development.Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology.Isoxazole-Derived Amino Acids are Bromodomain-Binding Acetyl-Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3.1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction.Cation-π interactions in CREBBP bromodomain inhibition: an electrostatic model for small-molecule binding affinity and selectivity.Pharmacophore-based virtual screening, molecular docking, molecular dynamics simulation, and biological evaluation for the discovery of novel BRD4 inhibitors.Tandem Chemoselective Suzuki-Miyaura Cross-Coupling Enabled by Nucleophile Speciation Control.Induction of apoptosis and downregulation of ERα in DMBA-induced mammary gland tumors in Sprague-Dawley rats by synthetic 3,5-disubstituted isoxazole derivatives.Discovery of BET bromodomain inhibitors and their role in target validation A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c5sc03115j.Direct photocapture of bromodomains using tropolone chemical probes Synthesis and cellular bioactivities of novel isoxazole derivatives incorporating an arylpiperazine moiety as anticancer agents

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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

http://www.wikidata.org/entity/Q27676915

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2013 nî lūn-bûn

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2013 թուականի Ապրիլին հրատարակուած գիտական յօդուած

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2013 թվականի ապրիլին հրատարակված գիտական հոդված

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2013年の論文

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2013年論文

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2013年論文

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2013年論文

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2013年論文

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2013年論文

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2013年论文

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name

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

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Journal of Medicinal Chemistry

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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

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Alison J Ritchie

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Andrew Gill

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Anthony Tumber

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Christopher Wells

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David W Sheppard

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Katherine Freeman

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Monica M Olcina

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Paul E Brennan

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Sarah Martin

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P2860

Selective inhibition of BET bromodomains

Histone recognition and large-scale structural analysis of the human bromodomain family

Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition

ACETYLATION AND METHYLATION OF HISTONES AND THEIR POSSIBLE ROLE IN THE REGULATION OF RNA SYNTHESIS

Molecular recognition at the active site of catechol-o-methyltransferase: energetically favorable replacement of a water molecule imported by a bisubstrate inhibitor

Suppression of inflammation by a synthetic histone mimic

Discovery and characterization of small molecule inhibitors of the BET family bromodomains

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery

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3217-27

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scholarly article

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4794388

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10.1021/JM301588R

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8

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56

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Panagis Filippakopoulos

Stuart J. Conway

Ester M Hammond

David S Hewings

Angela J Russell

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2013-04-25T00:00:00Z

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236069063

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23517011

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