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Developing irreversible inhibitors of the protein kinase cysteinome

Developing irreversible inhibitors of the protein kinase cysteinome

http://www.wikidata.org/entity/Q27027983

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Delineation of Polypharmacology across the Human Structural Kinome Using a Functional Site Interaction Fingerprint Approach Recent Advances in the Development and Application of Radiolabeled Kinase Inhibitors for PET Imaging Structure, Function, Pharmacology, and Therapeutic Potential of the G Protein, Gα/q,11 Combination Therapies to Inhibit the RAF/MEK/ERK Pathway in Melanoma: We are not Done Yet Ten things you should know about protein kinases: IUPHAR Review 14 Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery?Activated Ras as a Therapeutic Target: Constraints on Directly Targeting Ras Isoforms and Wild-Type versus Mutated Proteins Selective Inhibition of the Immunoproteasome by Structure-Based Targeting of a Non-catalytic Cysteine Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib Discovery of host-targeted covalent inhibitors of dengue virus Metabolically Labile Fumarate Esters Impart Kinetic Selectivity to Irreversible Inhibitors Chemical Proteomic Profiling of Human Methyltransferases Proteome-wide covalent ligand discovery in native biological systems The Tribbles 2 (TRB2) pseudokinase binds to ATP and autophosphorylates in a metal-independent manner Positive Allosteric Modulation of the Glucagon-like Peptide-1 Receptor by Diverse Electrophiles Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions Rationale for RAS mutation-tailored therapies.Pseudokinases: update on their functions and evaluation as new drug targets.The Concise Guide to PHARMACOLOGY 2013/14: enzymes.Homology modeling and ligand docking of Mitogen-activated protein kinase-activated protein kinase 5 (MK5).Discoidin domain receptors in disease.Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model.Irreversible inhibition of DNA polymerase β by small-molecule mimics of a DNA lesion Synergistic effects of various Her inhibitors in combination with IGF-1R, C-MET and Src targeting agents in breast cancer cell lines Determining Cysteines Available for Covalent Inhibition Across the Human Kinome.Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology.A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors.Design of reversible, cysteine-targeted Michael acceptors guided by kinetic and computational analysis.PAINS in the assay: chemical mechanisms of assay interference and promiscuous enzymatic inhibition observed during a sulfhydryl-scavenging HTS.A genetically encoded aza-Michael acceptor for covalent cross-linking of protein-receptor complexes.Pharmacological targeting of the pseudokinase Her3 Targeting a cryptic allosteric site for selective inhibition of the oncogenic protein tyrosine phosphatase Shp2 A novel CDK7 inhibitor of the Pyrazolotriazine class exerts broad-spectrum antiviral activity at nanomolar concentrations.Redox regulation of protein kinases.Identification of Covalent Bromodomain Binders through DNA Display of Small Molecules.Development of small molecules targeting the pseudokinase Her3.Prolonged and tunable residence time using reversible covalent kinase inhibitors.The ins and outs of selective kinase inhibitor development.Cell permeable affinity- and activity-based probes.Designing Irreversible Inhibitors--Worth the Effort?

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P2860

Developing irreversible inhibitors of the protein kinase cysteinome

http://www.wikidata.org/entity/Q27027983

description

2013 nî lūn-bûn

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2013 թուականի Փետրուարին հրատարակուած գիտական յօդուած

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2013 թվականի փետրվարին 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

@zh-cn

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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name

Developing irreversible inhibitors of the protein kinase cysteinome

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Developing irreversible inhibitors of the protein kinase cysteinome

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Developing irreversible inhibitors of the protein kinase cysteinome

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Developing irreversible inhibitors of the protein kinase cysteinome

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Developing irreversible inhibitors of the protein kinase cysteinome

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Developing irreversible inhibitors of the protein kinase cysteinome

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Developing irreversible inhibitors of the protein kinase cysteinome

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Developing irreversible inhibitors of the protein kinase cysteinome

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Developing irreversible inhibitors of the protein kinase cysteinome

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J.CHEMBIOL.2012.12.006

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Chemistry and Biology

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Developing irreversible inhibitors of the protein kinase cysteinome

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Lyn H. Jones

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Nathanael S. Gray

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Sara J. Buhrlage

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Tinghu Zhang

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Yogesh Sabnis

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Zheng Zhao

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Hallmarks of Cancer: The Next Generation

CLUSTAL W: improving the sensitivity of progressive multiple sequence alignment through sequence weighting, position-specific gap penalties and weight matrix choice

Binding of manumycin A inhibits IkappaB kinase beta activity

The protein kinase complement of the human genome

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

Beyond picomolar affinities: quantitative aspects of noncovalent and covalent binding of drugs to proteins

BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models

Structural biology contributions to the discovery of drugs to treat chronic myelogenous leukaemia

Role of a cysteine residue in the active site of ERK and the MAPKK family

Structures of Lung Cancer-Derived EGFR Mutants and Inhibitor Complexes: Mechanism of Activation and Insights into Differential Inhibitor Sensitivity

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