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Rational design of inhibitors that bind to inactive kinase conformations

Rational design of inhibitors that bind to inactive kinase conformations

http://www.wikidata.org/entity/Q29617558

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Structure prediction and validation of the ERK8 kinase domain Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors A conserved protonation-dependent switch controls drug binding in the Abl kinase Delineation of Polypharmacology across the Human Structural Kinome Using a Functional Site Interaction Fingerprint Approach Current targeted therapies in the treatment of advanced colorectal cancer: a review Somatic DNA mutation analysis in targeted therapy of solid tumours Charting a Path to Success in Virtual Screening JAK kinase targeting in hematologic malignancies: a sinuous pathway from identification of genetic alterations towards clinical indications Direct and Propagated Effects of Small Molecules on Protein-Protein Interaction Networks Kinases as druggable targets in trypanosomatid protozoan parasites Targeting cyclin-dependent kinases in human cancers: from small molecules to Peptide inhibitors Ten things you should know about protein kinases: IUPHAR Review 14 Biochemical and structural aspects of the ATP-binding domain in inflammasome-forming human NLRP proteins Discoidin domain receptor 1 (DDR1) kinase as target for structure-based drug discovery Rational approaches to improving selectivity in drug design Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery?Developing irreversible inhibitors of the protein kinase cysteinome Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation Structural biology contributions to the discovery of drugs to treat chronic myelogenous leukaemia Structure and regulation of the human Nek2 centrosomal kinase A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase Small Molecule Recognition of c-Src via the Imatinib-Binding Conformation Insights into the Conformational Variability and Regulation of Human Nek2 Kinase Structural Characterization of Proline-rich Tyrosine Kinase 2 (PYK2) Reveals a Unique (DFG-out) Conformation and Enables Inhibitor Design Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR , Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants Structural and mechanistic basis for a new mode of glycosyltransferase inhibition Cyclic AMP Analog Blocks Kinase Activation by Stabilizing Inactive Conformation: Conformational Selection Highlights a New Concept in Allosteric Inhibitor Design Genetic and Pharmacological Inhibition of PDK1 in Cancer Cells: CHARACTERIZATION OF A SELECTIVE ALLOSTERIC KINASE INHIBITOR Structural Basis for Selective Small Molecule Kinase Inhibition of Activated c-Met Discovery of a Potential Allosteric Ligand Binding Site in CDK2 A Novel Mode of Protein Kinase Inhibition Exploiting Hydrophobic Motifs of Autoinhibited Kinases: DISCOVERY OF ATP-INDEPENDENT INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR Conformational Control Inhibition of the BCR-ABL1 Tyrosine Kinase, Including the Gatekeeper T315I Mutant, by the Switch-Control Inhibitor DCC-2036 Briefly Bound to Activate: Transient Binding of a Second Catalytic Magnesium Activates the Structure and Dynamics of CDK2 Kinase for Catalysis Insights into the inhibition of the p90 ribosomal S6 kinase (RSK) by the flavonol glycoside SL0101 from the 1.5 Å crystal structure of the N-terminal domain of RSK2 with bound inhibitor.The R1275Q Neuroblastoma Mutant and Certain ATP-competitive Inhibitors Stabilize Alternative Activation Loop Conformations of Anaplastic Lymphoma Kinase X-ray crystal structure of bone marrow kinase in the x chromosome: a Tec family kinase Affinity-Based Probes Based on Type II Kinase Inhibitors

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Rational design of inhibitors that bind to inactive kinase conformations

http://www.wikidata.org/entity/Q29617558

description

2006 nî lūn-bûn

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2006 թուականի Յուլիսին հրատարակուած գիտական յօդուած

@hyw

2006 թվականի հուլիսին հրատարակված գիտական հոդված

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2006年の論文

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2006年論文

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2006年論文

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2006年論文

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2006年論文

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2006年論文

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2006年论文

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name

Rational design of inhibitors that bind to inactive kinase conformations

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Rational design of inhibitors that bind to inactive kinase conformations

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type

label

Rational design of inhibitors that bind to inactive kinase conformations

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Rational design of inhibitors that bind to inactive kinase conformations

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prefLabel

Rational design of inhibitors that bind to inactive kinase conformations

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Rational design of inhibitors that bind to inactive kinase conformations

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Nature Chemical Biology

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Rational design of inhibitors that bind to inactive kinase conformations

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Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis.

Exploiting structural principles to design cyclin-dependent kinase inhibitors.

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358-64

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scholarly article

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546894

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10.1038/NCHEMBIO799

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7001209

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1050699600

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16783341

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