JAK2 V617F constitutive activation requires JH2 residue F595: a pseudokinase domain target for specific inhibitors
about
JAK kinase targeting in hematologic malignancies: a sinuous pathway from identification of genetic alterations towards clinical indicationsCrystal structures of the JAK2 pseudokinase domain and the pathogenic mutant V617FStructure of a pseudokinase-domain switch that controls oncogenic activation of Jak kinasesModulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode DependentStructure of the pseudokinase-kinase domains from protein kinase TYK2 reveals a mechanism for Janus kinase (JAK) autoinhibitionPseudokinases: update on their functions and evaluation as new drug targets.Molecular basis for pseudokinase-dependent autoinhibition of JAK2 tyrosine kinase.Oncogenic JAK1 and JAK2-activating mutations resistant to ATP-competitive inhibitors.The molecular regulation of Janus kinase (JAK) activationThe constitutive activation of Jak2-V617F is mediated by a π stacking mechanism involving phenylalanines 595 and 617.Ab initio modeling and experimental assessment of Janus Kinase 2 (JAK2) kinase-pseudokinase complex structure.PDGF-D expression is down-regulated by TGFβ in fibroblastsATP binding to the pseudokinase domain of JAK2 is critical for pathogenic activationMolecular insights into regulation of JAK2 in myeloproliferative neoplasmsContribution of JAK2 mutations to T-cell lymphoblastic lymphoma development.Uncoupling JAK2 V617F activation from cytokine-induced signalling by modulation of JH2 αC helix.JAK2 mutants (e.g., JAK2V617F) and their importance as drug targets in myeloproliferative neoplasmsMolecular determinants of pathogenesis and clinical phenotype in myeloproliferative neoplasms.JAK2 inhibitors: what's the true therapeutic potential?Nuclear JAK2: form and function in cancer.A structure-function perspective of Jak2 mutations and implications for alternate drug design strategies: the road not taken.JAK2 inhibitors: are they the solution?Activating Janus kinase pseudokinase domain mutations in myeloproliferative and other blood cancers.The JAK-STAT pathway and hematopoietic stem cells from the JAK2 V617F perspective.Going for broke: targeting the human cancer pseudokinome.Oncogenic Drivers in Myeloproliferative Neoplasms: From JAK2 to Calreticulin Mutations.What Do Molecular Tests Add to Prognostic Stratification in MF: Is It Time to Add These to Our Clinical Practice?Multiple oligomerization domains of KANK1-PDGFRβ are required for JAK2-independent hematopoietic cell proliferation and signaling via STAT5 and ERK.Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases.A shift in the salt bridge interaction of residues D620 and E621 mediates the constitutive activation of Jak2-H538Q/K539L.Mechanistic Insights into Regulation of JAK2 Tyrosine Kinase.Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders.
P2860
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P2860
JAK2 V617F constitutive activation requires JH2 residue F595: a pseudokinase domain target for specific inhibitors
description
2010 nî lūn-bûn
@nan
2010 թուականի Յունիսին հրատարակուած գիտական յօդուած
@hyw
2010 թվականի հունիսին 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
JAK2 V617F constitutive activa ...... target for specific inhibitors
@ast
JAK2 V617F constitutive activa ...... target for specific inhibitors
@en
type
label
JAK2 V617F constitutive activa ...... target for specific inhibitors
@ast
JAK2 V617F constitutive activa ...... target for specific inhibitors
@en
prefLabel
JAK2 V617F constitutive activa ...... target for specific inhibitors
@ast
JAK2 V617F constitutive activa ...... target for specific inhibitors
@en
P2093
P2860
P1433
P1476
JAK2 V617F constitutive activa ...... target for specific inhibitors
@en
P2093
Alexandra Dusa
Christian Pecquet
Céline Mouton
Murielle Herman
P2860
P304
P356
10.1371/JOURNAL.PONE.0011157
P407
P577
2010-06-16T00:00:00Z