Reactome | Imatinib-resistant KIT mutants do not bind imatinib

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Imatinib-resistant KIT mutants do not bind imatinib Show undefined attributes

authored	[InstanceEdit:9681395] Rothfels, Karen, 2020-04-01
category	transition
compartment	[Compartment:876] plasma membrane
created	[InstanceEdit:9669858] Rothfels, Karen, 2019-12-03
crossReference	[DatabaseIdentifier:12020745] Mondo:0004992
dbId	9669859
disease	[Disease:1500689] cancer
displayName	Imatinib-resistant KIT mutants do not bind imatinib
edited	[InstanceEdit:9686618] Rothfels, Karen, 2020-05-04
entityFunctionalStatus	[EntityFunctionalStatus:9669860] loss_of_function of imatinib resistant KIT mutants [plasma membrane]
eventOf	[Pathway:R-HSA-9669917] Imatinib-resistant KIT mutants - Homo sapiens
input	[ChemicalDrug:R-ALL-9659761] imatinib [cytosol] [DefinedSet:R-HSA-9669748] imatinib resistant KIT mutants [plasma membrane]
isChimeric	false
isInDisease	true
isInferred	false
literatureReference	[LiteratureReference:9670475] Juxtamembrane mutant V560GKit is more sensitive to Imatinib (STI571) compared with wild-type c-kit whereas the kinase domain mutant D816VKit is resistant [LiteratureReference:9671417] Resistance to c-KIT kinase inhibitors conferred by V654A mutation [LiteratureReference:9669031] A missense mutation in KIT kinase domain 1 correlates with imatinib resistance in gastrointestinal stromal tumors [LiteratureReference:9671373] Molecular basis of the constitutive activity and STI571 resistance of Asp816Val mutant KIT receptor tyrosine kinase [LiteratureReference:9669117] Functional analyses and molecular modeling of two c-Kit mutations responsible for imatinib secondary resistance in GIST patients [LiteratureReference:9669211] KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients [LiteratureReference:9669165] Imatinib binding and cKIT inhibition is abrogated by the cKIT kinase domain I missense mutation Val654Ala [LiteratureReference:9670319] Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients [LiteratureReference:9669094] Complementary activity of tyrosine kinase inhibitors against secondary kit mutations in imatinib-resistant gastrointestinal stromal tumours [LiteratureReference:9669259] The role of small molecule Kit protein-tyrosine kinase inhibitors in the treatment of neoplastic disorders [LiteratureReference:9669232] Secondary KIT mutations: the GIST of drug resistance and sensitivity [LiteratureReference:9671447] Structural and clinical consequences of activation loop mutations in class III receptor tyrosine kinases [LiteratureReference:9673518] Gastrointestinal stromal tumours: origin and molecular oncology [LiteratureReference:9680569] Novel Insights into the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors
maxDepth	1
modified	[InstanceEdit:9830342] Matthews, Lisa, 2023-03-08
name	Imatinib-resistant KIT mutants do not bind imatinib
normalReaction	[Reaction:R-HSA-9669854] KIT binds type II TKIs
releaseDate	2020-06-10
reviewStatus	[ReviewStatus:9821382] five stars
reviewed	[InstanceEdit:9678239] Serrano, C�sar, 2020-03-13 [InstanceEdit:9678232] Garc�a-Valverde, Alfonso, 2020-03-13 [InstanceEdit:9678237] Pilco-Janeta, Daniel, 2020-03-13
schemaClass	FailedReaction
species	[Species:48887] Homo sapiens
stId	R-HSA-9669859
summation	[Summation:9671475] Although most exon 11 mutations in the KIT receptor are sens...

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[Pathway:R-HSA-9669917] Imatinib-resistant KIT mutants

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