Structural and thermodynamic characterization of the TYK2 and JAK3 kinase domains in complex with CP-690550 and CMP-6
about
Crystal structures of the JAK2 pseudokinase domain and the pathogenic mutant V617FEnabling structure-based drug design of Tyk2 through co-crystallization with a stabilizing aminoindazole inhibitorStructure of the pseudokinase-kinase domains from protein kinase TYK2 reveals a mechanism for Janus kinase (JAK) autoinhibitionTYK2 kinase activity is required for functional type I interferon responses in vivoTofacitinib and analogs as inhibitors of the histone kinase PRK1 (PKN1).High-precision isothermal titration calorimetry with automated peak-shape analysis.Adapter protein Shc regulates Janus kinase 3 phosphorylationIdentification of small molecule inhibitors of phosphatidylinositol 3-kinase and autophagy.Crystal structures of PRK1 in complex with the clinical compounds lestaurtinib and tofacitinib reveal ligand induced conformational changes.EGCG enhances the therapeutic potential of gemcitabine and CP690550 by inhibiting STAT3 signaling pathway in human pancreatic cancer.Applications of isothermal titration calorimetry in pure and applied research--survey of the literature from 2010.Structure-based design of oxygen-linked macrocyclic kinase inhibitors: discovery of SB1518 and SB1578, potent inhibitors of Janus kinase 2 (JAK2) and Fms-like tyrosine kinase-3 (FLT3).Tofacitinib for the treatment of rheumatoid arthritis.Identification of molecular switch regulating interactions of Janus kinase 3 with cytoskeletal proteins.A displaced-solvent functional analysis of model hydrophobic enclosures.Novel hinge-binding motifs for Janus kinase 3 inhibitors: a comprehensive structure-activity relationship study on tofacitinib bioisosteres.FERM domain mutations induce gain of function in JAK3 in adult T-cell leukemia/lymphomaThe molecular basis of IL-10 function: from receptor structure to the onset of signaling.MoNetFamily: a web server to infer homologous modules and module-module interaction networks in vertebratesEstablishing the role of tyrosine kinase 2 in cancer.Comparative analysis of the human and zebrafish kinomes: focus on the development of kinase inhibitors.Biology and significance of the JAK/STAT signalling pathways.The use of structural biology in Janus kinase targeted drug discovery.Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F.STAT3 genotypic variation and cellular STAT3 activation and colon leukocyte recruitment in pediatric Crohn disease.JAK inhibitor tofacitinib for treating rheumatoid arthritis: from basic to clinical.Approaches to efficiently estimate solvation and explicit water energetics in ligand binding: the use of WaterMap.Therapeutic potential of tyrosine kinase 2 in autoimmunity.Efficacy and safety of tofacitinib for active rheumatoid arthritis with an inadequate response to methotrexate or disease-modifying antirheumatic drugs: a meta-analysis of randomized controlled trials.Selective JAK inhibitors.Progress toward JAK1-selective inhibitors.Oxindole-based SYK and JAK3 dual inhibitors for rheumatoid arthritis: designing, synthesis and biological evaluation.Inhibitor-based affinity probes for the investigation of JAK signaling pathways.Convergent mutations and kinase fusions lead to oncogenic STAT3 activation in anaplastic large cell lymphoma.Tricyclic covalent inhibitors selectively target Jak3 through an active site thiol.Resolving TYK2 locus genotype-to-phenotype differences in autoimmunity.Enhancing specificity in the Janus kinases: a study on the thienopyridine JAK2 selective mechanism combined molecular dynamics simulation.Structural snapshots of full-length Jak1, a transmembrane gp130/IL-6/IL-6Rα cytokine receptor complex, and the receptor-Jak1 holocomplex.Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket.Global connectivity of hub residues in Oncoprotein structures encodes genetic factors dictating personalized drug response to targeted Cancer therapy.
P2860
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P2860
Structural and thermodynamic characterization of the TYK2 and JAK3 kinase domains in complex with CP-690550 and CMP-6
description
2010 nî lūn-bûn
@nan
2010 թուականի Յուլիսին հրատարակուած գիտական յօդուած
@hyw
2010 թվականի հուլիսին հրատարակված գիտական հոդված
@hy
2010年の論文
@ja
2010年論文
@yue
2010年論文
@zh-hant
2010年論文
@zh-hk
2010年論文
@zh-mo
2010年論文
@zh-tw
2010年论文
@wuu
name
Structural and thermodynamic c ...... mplex with CP-690550 and CMP-6
@ast
Structural and thermodynamic c ...... mplex with CP-690550 and CMP-6
@en
Structural and thermodynamic c ...... mplex with CP-690550 and CMP-6
@nl
type
label
Structural and thermodynamic c ...... mplex with CP-690550 and CMP-6
@ast
Structural and thermodynamic c ...... mplex with CP-690550 and CMP-6
@en
Structural and thermodynamic c ...... mplex with CP-690550 and CMP-6
@nl
prefLabel
Structural and thermodynamic c ...... mplex with CP-690550 and CMP-6
@ast
Structural and thermodynamic c ...... mplex with CP-690550 and CMP-6
@en
Structural and thermodynamic c ...... mplex with CP-690550 and CMP-6
@nl
P2093
P1476
Structural and thermodynamic c ...... mplex with CP-690550 and CMP-6
@en
P2093
Akshay Patny
Alfredo G Tomasselli
Brian Korniski
Cynthia D Sommers
E J Jacobsen
H David Fischer
Horng-Chih Huang
Iris K Leung
Jacqueline E Day
James R Kiefer
P304
P356
10.1016/J.JMB.2010.05.020
P407
P577
2010-07-16T00:00:00Z