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Details on Person Imatinib-resistant PDGFR mutants don't bind imatinib

Class:Id	FailedReaction:9674397
_displayName	Imatinib-resistant PDGFR mutants don't bind imatinib
_doRelease	TRUE
_timestamp	2020-02-27 15:47:09
authored	[InstanceEdit:9677035] Rothfels, Karen, 2020-02-25
compartment	[Compartment:876] plasma membrane [Compartment:70101] cytosol
created	[InstanceEdit:9674407] Rothfels, Karen, 2020-01-13
disease	[Disease:1500689] cancer
edited	[InstanceEdit:9677035] Rothfels, Karen, 2020-02-25
entityFunctionalStatus	[EntityFunctionalStatus:9674394] loss_of_function of imatinib-resistant PDGFR mutants [plasma membrane]
input	[DefinedSet:9672125] imatinib-resistant PDGFR mutants [plasma membrane] [Homo sapiens] [ChemicalDrug:9659761] imatinib [cytosol]
isChimeric	FALSE
literatureReference	[LiteratureReference:9671898] PDGFRA activating mutations in gastrointestinal stromal tumors [LiteratureReference:9671911] PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib [LiteratureReference:9672488] A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome [LiteratureReference:9673573] Sorafenib is a potent inhibitor of FIP1L1-PDGFRalpha and the imatinib-resistant FIP1L1-PDGFRalpha T674I mutant [LiteratureReference:9673492] A novel FIP1L1-PDGFRA mutant destabilizing the inactive conformation of the kinase domain in chronic eosinophilic leukemia/hypereosinophilic syndrome [LiteratureReference:9673563] Primary resistance to imatinib in Fip1-like 1-platelet-derived growth factor receptor alpha-positive eosinophilic leukemia [LiteratureReference:9671429] Sorafenib inhibits many kinase mutations associated with drug-resistant gastrointestinal stromal tumors [LiteratureReference:9671319] A precision therapy against cancers driven by KIT/PDGFRA mutations [LiteratureReference:9674274] Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants [LiteratureReference:9671447] Structural and clinical consequences of activation loop mutations in class III receptor tyrosine kinases [LiteratureReference:9673583] The role of small molecule platelet-derived growth factor receptor (PDGFR) inhibitors in the treatment of neoplastic disorders
modified	[InstanceEdit:9674505] Rothfels, Karen, 2020-01-13 [InstanceEdit:9676111] Rothfels, Karen, 2020-02-07 [InstanceEdit:9676121] Rothfels, Karen, 2020-02-08 [InstanceEdit:9676333] Rothfels, Karen, 2020-02-12 [InstanceEdit:9677115] Rothfels, Karen, 2020-02-27 [InstanceEdit:9830342] Matthews, Lisa, 2023-03-08
name	Imatinib-resistant PDGFR mutants don't bind imatinib
normalReaction	[Reaction:9674095] PDGFRs bind type II TKI [Homo sapiens]
releaseDate	2020-03-17
reviewed	[InstanceEdit:9676030] Ip, Carman K M, 2020-02-06
reviewStatus	[ReviewStatus:9821382] five stars
species	[Species:48887] Homo sapiens
stableIdentifier	[StableIdentifier:9674423] R-HSA-9674397.2
summation	[Summation:9674405] PDGFRA mutations that are resistant to imatinib include poin...
(hasEvent)	[Pathway:9674396] Imatinib-resistant PDGFR mutants [Homo sapiens]
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