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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

http://www.wikidata.org/entity/Q27677115

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Covalent docking of large libraries for the discovery of chemical probes Proteome-wide covalent ligand discovery in native biological systems Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions Targeting Non-Catalytic Cysteine Residues Through Structure-Guided Drug Discovery Determining Cysteines Available for Covalent Inhibition Across the Human Kinome.Design of reversible, cysteine-targeted Michael acceptors guided by kinetic and computational analysis.A fragment-based method to discover irreversible covalent inhibitors of cysteine proteases.Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility.A binding hotspot in Trypanosoma cruzi histidyl-tRNA synthetase revealed by fragment-based crystallographic cocktail screens.Prolonged and tunable residence time using reversible covalent kinase inhibitors.Covalent targeting of acquired cysteines in cancer Pharmacokinetics and pharmacodynamics of orally administered acetylenic tricyclic bis(cyanoenone), a highly potent Nrf2 activator with a reversible covalent mode of action.Covalent Tethering of Fragments For Covalent Probe Discovery Kinase inhibitors as potential agents in the treatment of multiple myeloma.Signal transduction: From the atomic age to the post-genomic era Targeting protein kinases with selective and semipromiscuous covalent inhibitors.Privileged scaffolds in lead generation.The Search for Covalently Ligandable Proteins in Biological Systems.Covalent EGFR Inhibitors: Binding Mechanisms, Synthetic Approaches, and Clinical Profiles.Targeted Covalent Inhibitors for Drug Design.Targeting biomolecules with reversible covalent chemistry Hot-spot identification on a broad class of proteins and RNA suggest unifying principles of molecular recognition.Chromatin Kinases Act on Transcription Factors and Histone Tails in Regulation of Inducible Transcription Thiophene bridged aldehydes (TBAs) image ALDH activity in cells via modulation of intramolecular charge transfer.Facile synthesis of borofragments and their evaluation in activity-based protein profiling.Differential control of Toll-like receptor 4-induced interleukin-10 induction in macrophages and B cells reveals a role for p90 ribosomal S6 kinases.Current perspectives in fragment-based lead discovery (FBLD).Tandem Wittig/Diels-Alder diversification of genetically encoded peptide libraries.Design, synthesis, and cytotoxic evaluation of novel scopoletin derivatives.What Do Reactive Fragments Actually Do in Cells?Characterization of Covalent-Reversible EGFR Inhibitors.CavityPlus: a web server for protein cavity detection with pharmacophore modelling, allosteric site identification and covalent ligand binding ability prediction.The Taxonomy of Covalent Inhibitors Protein-ligand (un)binding kinetics as a new paradigm for drug discovery at the crossroad between experiments and modelling Target-based drug discovery through inversion of quantitative structure-drug-property relationships and molecular simulation: CA IX-sulphonamide complexes

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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

http://www.wikidata.org/entity/Q27677115

description

2013 nî lūn-bûn

@nan

2013 թուականի Ապրիլին հրատարակուած գիտական յօդուած

@hyw

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

Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

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Journal of the American Chemical Society

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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

@en

P2093

Iana M Serafimova

http://www.w3.org/2001/XMLSchema#string

Jack Taunton

http://www.w3.org/2001/XMLSchema#string

Rand M Miller

http://www.w3.org/2001/XMLSchema#string

Shyam Krishnan

http://www.w3.org/2001/XMLSchema#string

Ville O Paavilainen

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P2860

Mitogen- and stress-activated protein kinase-1 (MSK1) is directly activated by MAPK and SAPK2/p38, and may mediate activation of CREB

MSK1 and MSK2 are required for the mitogen- and stress-induced phosphorylation of CREB and ATF1 in fibroblasts

Site-directed ligand discovery

Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension

Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity

Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine

Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors

Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles

Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor

Targeting cancer with small molecule kinase inhibitors

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5298-301

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scholarly article

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4772289

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10.1021/JA401221B

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14

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135

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2013-04-10T00:00:00Z

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23540679

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3665406

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