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

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

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

http://www.wikidata.org/entity/Q27674710

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ZMYND11 links histone H3.3K36me3 to transcription elongation and tumour suppression Design of small molecule epigenetic modulators The bromodomain: from epigenome reader to druggable target Cancer epigenetics drug discovery and development: the challenge of hitting the mark Protein lysine acetylation by p300/CBP Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors Naphthyridines as novel BET family bromodomain inhibitors Different orientations of low-molecular-weight fragments in the binding pocket of a BRD4 bromodomain 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading 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 Targeting BET bromodomains for cancer treatment An Epigenetic Compound Library Screen Identifies BET Inhibitors That Promote HSV-1 and -2 Replication by Bridging P-TEFb to Viral Gene Promoters through BRD4 Identification of novel potent human testis-specific and bromodomain-containing protein (BRDT) inhibitors using crystal structure-based virtual screening Drug Discovery Targeting Bromodomain-Containing Protein 4.Selective BET bromodomain inhibition as an antifungal therapeutic strategy Seeding collaborations to advance kinase science with the GSK Published Kinase Inhibitor Set (PKIS)Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains Target validation using chemical probes.PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains BET bromodomain inhibitors: a patent review.Small-molecule modulators for epigenetics targets.Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching.High-throughput single-molecule screen for small-molecule perturbation of splicing and transcription kinetics.Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk.Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability.Large-Scale Computational Screening Identifies First in Class Multitarget Inhibitor of EGFR Kinase and BRD4.BRD4 is a novel therapeutic target for liver fibrosis.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.Targeting the chromatin remodeling enzyme BRG1 increases the efficacy of chemotherapy drugs in breast cancer cells Phenotypic screening and fragment-based approaches to the discovery of small-molecule bromodomain ligands.Bromodomains and their pharmacological inhibitors.Selective Inhibition of CBX6: A Methyllysine Reader Protein in the Polycomb Family

P2860

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P2860

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

http://www.wikidata.org/entity/Q27674710

description

2012 nî lūn-bûn

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2012 թուականի Նոյեմբերին հրատարակուած գիտական յօդուած

@hyw

2012 թվականի նոյեմբերին հրատարակված գիտական հոդված

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2012年の論文

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2012年論文

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2012年論文

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2012年論文

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2012年論文

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2012年論文

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2012年论文

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Identification of a Chemical P ...... tion of a Fragment-Derived Hit

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Identification of a Chemical P ...... tion of a Fragment-Derived Hit

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Andrew S Cook

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Brian Marsden

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Brian S Gerstenberger

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Dafydd R Owen

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Gerwyn Bish

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John D Trzupek

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Karl Nocka

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Mark E Bunnage

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Martin Philpott

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Michael J Primiano

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P2860

Translating the Histone Code

Selective inhibition of BET bromodomains

Brd4 coactivates transcriptional activation of NF-kappaB via specific binding to acetylated RelA

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

NUT midline carcinoma

Brd4 links chromatin targeting to HPV transcriptional silencing

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

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

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10.1021/JM3010515

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22

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55

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Panagis Filippakopoulos

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