Reactome | PDGFRs bind type II TKI

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PDGFRs bind type II TKI Show undefined attributes

authored	[InstanceEdit:9677035] Rothfels, Karen, 2020-02-25
category	binding
compartment	[Compartment:876] plasma membrane [Compartment:70101] cytosol
created	[InstanceEdit:9674096] Rothfels, Karen, 2020-01-10
dbId	9674095
diseaseReaction	[Reaction:R-HSA-9674430] PDGFR mutants bind type II TKIs - Homo sapiens [FailedReaction:R-HSA-9674397] Imatinib-resistant PDGFR mutants don't bind imatinib - Homo sapiens [FailedReaction:R-HSA-9674414] Sorafenib-resistant PDGFR mutants don't bind sorefenib - Homo sapiens [FailedReaction:R-HSA-9674398] D842V PDGFRA doesn't bind sunitinib - Homo sapiens [FailedReaction:R-HSA-9674408] Regorafenib-resistant PDGFR mutants don't bind regorafenib - Homo sapiens
displayName	PDGFRs bind type II TKI
edited	[InstanceEdit:9677035] Rothfels, Karen, 2020-02-25
eventOf	[Pathway:R-HSA-186797] Signaling by PDGF - Homo sapiens
input	[DefinedSet:R-HSA-186792] PDGFRA, PDGFRB [plasma membrane] [DefinedSet:R-ALL-9674079] type II PDGFR-binding tyrosine kinase inhibitors [cytosol]
isChimeric	false
isInDisease	false
isInferred	false
literatureReference	[LiteratureReference:9674200] Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays [LiteratureReference:9674255] Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib) [LiteratureReference:2077545] E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition [LiteratureReference:9674254] Inhibition of PDGF, TGF-?, and Abl signaling and reduction of liver fibrosis by the small molecule Bcr-Abl tyrosine kinase antagonist Nilotinib [LiteratureReference:9674181] BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy [LiteratureReference:9674295] Triple Angiokinase Inhibitor Nintedanib Directly Inhibits Tumor Cell Growth and Induces Tumor Shrinkage via Blocking Oncogenic Receptor Tyrosine Kinases [LiteratureReference:9674174] BAY 43-9006: preclinical data [LiteratureReference:9674258] Preclinical and clinical development of the oral multikinase inhibitor sorafenib in cancer treatment [LiteratureReference:9674233] In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship [LiteratureReference:9674288] Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor [LiteratureReference:9673583] The role of small molecule platelet-derived growth factor receptor (PDGFR) inhibitors in the treatment of neoplastic disorders [LiteratureReference:9674290] The PDGF/PDGFR pathway as a drug target [LiteratureReference:9674274] Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants
maxDepth	1
modified	[InstanceEdit:10914110] Weiser, Joel, 2026-03-16
name	PDGFRs bind type II TKI
orthologousEvent	[Reaction:R-DME-9674095] PDGFRs bind type II TKI - Drosophila melanogaster [Reaction:R-CEL-9674095] PDGFRs bind type II TKI - Caenorhabditis elegans [Reaction:R-GGA-9674095] PDGFRs bind type II TKI - Gallus gallus [Reaction:R-XTR-9674095] PDGFRs bind type II TKI - Xenopus tropicalis [Reaction:R-DRE-9674095] PDGFRs bind type II TKI - Danio rerio [Reaction:R-SSC-9674095] PDGFRs bind type II TKI - Sus scrofa [Reaction:R-BTA-9674095] PDGFRs bind type II TKI - Bos taurus [Reaction:R-CFA-9674095] PDGFRs bind type II TKI - Canis familiaris [Reaction:R-RNO-9674095] PDGFRs bind type II TKI - Rattus norvegicus [Reaction:R-MMU-9674095] PDGFRs bind type II TKI - Mus musculus
output	[Complex:R-HSA-9674086] PDGFR:type II PDGFR-binding TKIs [plasma membrane]
releaseDate	2020-03-17
reviewStatus	[ReviewStatus:9821382] five stars
reviewed	[InstanceEdit:9676030] Ip, Carman K M, 2020-02-06
schemaClass	Reaction
species	[Species:48887] Homo sapiens
stId	R-HSA-9674095
summation	[Summation:9674091] Wild-type PDGFRA and PDGFRB can be bound and inhibited by cl...

Referrals

(normalReaction)	[Reaction:R-HSA-9674430] PDGFR mutants bind type II TKIs [FailedReaction:R-HSA-9674397] Imatinib-resistant PDGFR mutants don't bind imatinib [FailedReaction:R-HSA-9674414] Sorafenib-resistant PDGFR mutants don't bind sorefenib [FailedReaction:R-HSA-9674398] D842V PDGFRA doesn't bind sunitinib [FailedReaction:R-HSA-9674408] Regorafenib-resistant PDGFR mutants don't bind regorafenib
(hasEvent)	[Pathway:R-HSA-186797] Signaling by PDGF

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