[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains - Wikidata - wikimedia - TriplyDB

[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains

[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains

http://www.wikidata.org/entity/Q34390229

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The bromodomain: from epigenome reader to druggable target Protein lysine acetylation by p300/CBP NMR Fragment Screening Hit Induces Plasticity of BRD7/9 Bromodomains Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor Targeting BET bromodomains for cancer treatment LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor Binding hotspots of BAZ2B bromodomain: Histone interaction revealed by solution NMR driven docking.Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk.Large-Scale Computational Screening Identifies First in Class Multitarget Inhibitor of EGFR Kinase and BRD4.Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.Discovery of a PCAF Bromodomain Chemical Probe.Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF.Progress in the Development of non-BET Bromodomain Chemical Probes.Toward personalized management in bladder cancer: the promise of novel molecular taxonomy.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.Structural features and inhibitors of bromodomains.9H-purine scaffold reveals induced-fit pocket plasticity of the BRD9 bromodomain Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.Identification of a Novel Class of BRD4 Inhibitors by Computational Screening and Binding Simulations.Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex.A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction.Chemical probes and inhibitors of bromodomains outside the BET family.What is the future of bromodomains in targeted drug development?A computational insight into binding modes of inhibitors XD29, XD35, and XD28 to bromodomain-containing protein 4 based on molecular dynamics simulations.Activity of bromodomain protein inhibitors/binders against asexual-stage Plasmodium falciparum parasites.Triazolophthalazines: Easily Accessible Compounds with Potent Antitubercular Activity.Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains 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.Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatography Discovery of a PCAF Bromodomain Chemical Probe

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[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains

http://www.wikidata.org/entity/Q34390229

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2013 nî lūn-bûn

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2013 թուականի Դեկտեմբերին հրատարակուած գիտական յօդուած

@hyw

2013 թվականի դեկտեմբերին հրատարակված գիտական հոդված

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2013年の論文

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2013年学术文章

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2013年学术文章

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2013年学术文章

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2013年学术文章

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2013年学术文章

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2013年學術文章

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Journal of Medicinal Chemistry

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[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains

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Brian D Marsden

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Chris Wells

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Clarence Yapp

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Hannah Lingard

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Ildiko Felletar

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Martin Philpott

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Octovia P Monteiro

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Oleg Fedorov

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Paul E Brennan

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Sarah J Martin

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Selective inhibition of BET bromodomains

Phospho switch triggers Brd4 chromatin binding and activator recruitment for gene-specific targeting

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

Suppression of inflammation by a synthetic histone mimic

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

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

Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides

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

Coot: model-building tools for molecular graphics

Automated protein model building combined with iterative structure refinement

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462-476

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10.1021/JM401568S

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2

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57

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Panagis Filippakopoulos

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2013-12-30T00:00:00Z

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259243903

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24313754

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