Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening
about
Comprehensive structural and functional characterization of the human kinome by protein structure modeling and ligand virtual screening.Structural determinants of PERK inhibitor potency and selectivityUsing free energy of binding calculations to improve the accuracy of virtual screening predictions.The Jak2 small molecule inhibitor, G6, reduces the tumorigenic potential of T98G glioblastoma cells in vitro and in vivo.Identification of novel SAR properties of the Jak2 small molecule inhibitor G6: significance of the para-hydroxyl orientationStructure-function correlation of G6, a novel small molecule inhibitor of Jak2: indispensability of the stilbenoid core.The constitutive activation of Jak2-V617F is mediated by a π stacking mechanism involving phenylalanines 595 and 617.The small molecule inhibitor G6 significantly reduces bone marrow fibrosis and the mutant burden in a mouse model of Jak2-mediated myelofibrosis.The stilbenoid tyrosine kinase inhibitor, G6, suppresses Jak2-V617F-mediated human pathological cell growth in vitro and in vivo.Cell death induced by the Jak2 inhibitor, G6, correlates with cleavage of vimentin filaments.The Jak2 inhibitor, G6, alleviates Jak2-V617F-mediated myeloproliferative neoplasia by providing significant therapeutic efficacy to the bone marrowA46, a benzothiophene-derived compound, suppresses Jak2-mediated pathologic cell growthThe recent medicinal chemistry development of Jak2 tyrosine kinase small molecule inhibitors.The use of structural biology in Janus kinase targeted drug discovery.Identification of myeloproliferative neoplasm drug agents via predictive simulation modeling: assessing responsiveness with micro-environment derived cytokines.Recent developments on JAK2 inhibitors: a patent review.How Does the L884P Mutation Confer Resistance to Type-II Inhibitors of JAK2 Kinase: A Comprehensive Molecular Modeling Study.The JAK2 pathway is activated in idiopathic pulmonary fibrosis.Identification of 8-Hydroxyquinoline Derivatives Active Against Somatic V658F Mutant JAK1-Dependent Cells.Jak2 Tyrosine Kinase: A Potential Therapeutic Target for AT1 Receptor Mediated Cardiovascular Disease.
P2860
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P2860
Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening
description
2009 nî lūn-bûn
@nan
2009 թուականի Մայիսին հրատարակուած գիտական յօդուած
@hyw
2009 թվականի մայիսին հրատարակված գիտական հոդված
@hy
2009年の論文
@ja
2009年論文
@yue
2009年論文
@zh-hant
2009年論文
@zh-hk
2009年論文
@zh-mo
2009年論文
@zh-tw
2009年论文
@wuu
name
Identification of a novel inhi ...... ucture-based virtual screening
@ast
Identification of a novel inhi ...... ucture-based virtual screening
@en
type
label
Identification of a novel inhi ...... ucture-based virtual screening
@ast
Identification of a novel inhi ...... ucture-based virtual screening
@en
prefLabel
Identification of a novel inhi ...... ucture-based virtual screening
@ast
Identification of a novel inhi ...... ucture-based virtual screening
@en
P2093
P2860
P50
P1476
Identification of a novel inhi ...... ucture-based virtual screening
@en
P2093
Annet Kirabo
Jacqueline Sayyah
Kenneth S Zuckerman
Kirpal S Bisht
Lubomir Sokol
Meghanath Gali
Nicholas C Figueroa
Peter P Sayeski
Róbert Kiss
P2860
P304
P356
10.1016/J.BMCL.2009.04.138
P407
P577
2009-05-05T00:00:00Z