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Entries
PDGFRs bind type II TKI
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authored
[InstanceEdit:9677035] Rothfels, Karen, 2020年02月25日
category
binding
compartment
[Compartment:876] plasma membrane
[Compartment:70101] cytosol
created
[InstanceEdit:9674096] Rothfels, Karen, 2020年01月10日
dbId
9674095
displayName
PDGFRs bind type II TKI
edited
[InstanceEdit:9677035] Rothfels, Karen, 2020年02月25日
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:10867632] Weiser, Joel, 2025年08月27日
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年03月17日
reviewStatus
[ReviewStatus:9821382] five stars
reviewed
[InstanceEdit:9676030] Ip, Carman K M, 2020年02月06日
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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