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Schema
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Reaction
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Entries
ERBB2 binds TKIs
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authored
[InstanceEdit:9656339] Orlic-Milacic, Marija, 2019-07-31
category
binding
compartment
[Compartment:70101] cytosol
[Compartment:876] plasma membrane
created
[InstanceEdit:9652267] Orlic-Milacic, Marija, 2019-06-28
dbId
9652264
diseaseReaction
[FailedReaction:R-HSA-9665304] ERBB2 T862A does not bind sapitinib - Homo sapiens
[FailedReaction:R-HSA-9665315] ERBB2 T733I does not bind tesevatinib - Homo sapiens
[FailedReaction:R-HSA-9665286] Resistant ERBB2 KD mutants do not bind neratinib - Homo sapiens
[FailedReaction:R-HSA-9665280] ERBB2 KD mutants do not bind osimertinib - Homo sapiens
[FailedReaction:R-HSA-9665311] ERBB2 T798M does not bind afatinib - Homo sapiens
[FailedReaction:R-HSA-9665278] Resistant ERBB2 KD mutants do not bind AEE788 - Homo sapiens
[FailedReaction:R-HSA-9665284] Resistant ERBB2 KD mutants do not bind lapatinib - Homo sapiens
[Reaction:R-HSA-9665412] ERBB2 ECD mutants bind TKIs - Homo sapiens
[Reaction:R-HSA-9665702] ERBB2 TMD/JMD mutants bind TKIs - Homo sapiens
displayName
ERBB2 binds TKIs
edited
[InstanceEdit:9665760] Orlic-Milacic, Marija, 2019-11-01
eventOf
[Pathway:R-HSA-9652282] Drug-mediated inhibition of ERBB2 signaling - Homo sapiens
[Pathway:R-HSA-9634285] Constitutive Signaling by Overexpressed ERBB2 - Homo sapiens
input
[Complex:R-HSA-1227970] ERBB2:ERBIN:HSP90:CDC37 [plasma membrane]
[DefinedSet:R-ALL-9652360] lapatinib, neratinib, afatinib, AZ5104, tesevatinib, canertinib, sapitinib, CP-724714, AEE78 [cytosol]
isChimeric
false
isInDisease
false
isInferred
false
literatureReference
[LiteratureReference:9652234] Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways
[LiteratureReference:9652252] A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells
[LiteratureReference:1237426] Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase
[LiteratureReference:9652226] BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models
[LiteratureReference:9647026] An Acquired
HER2
T798I
Gatekeeper Mutation Induces Resistance to Neratinib in a Patient with HER2 Mutant-Driven Breast Cancer
[LiteratureReference:9652237] Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647
[LiteratureReference:9652323] Akt, MAPK (Erk1/2), and p38 act in concert to promote apoptosis in response to ErbB receptor family inhibition
[LiteratureReference:9652320] AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: a unique agent for simultaneous ERBB receptor blockade in cancer
[LiteratureReference:9652336] Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor
[LiteratureReference:9652318] AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity
maxDepth
1
modified
[InstanceEdit:11051501] Weiser, Joel, 2026-03-16
name
ERBB2 binds TKIs
orthologousEvent
[Reaction:R-SPO-9652264] ERBB2 binds TKIs - Schizosaccharomyces pombe
[Reaction:R-CEL-9652264] ERBB2 binds TKIs - Caenorhabditis elegans
[Reaction:R-DME-9652264] ERBB2 binds TKIs - Drosophila melanogaster
[Reaction:R-GGA-9652264] ERBB2 binds TKIs - Gallus gallus
[Reaction:R-DRE-9652264] ERBB2 binds TKIs - Danio rerio
[Reaction:R-SSC-9652264] ERBB2 binds TKIs - Sus scrofa
[Reaction:R-BTA-9652264] ERBB2 binds TKIs - Bos taurus
[Reaction:R-CFA-9652264] ERBB2 binds TKIs - Canis familiaris
[Reaction:R-RNO-9652264] ERBB2 binds TKIs - Rattus norvegicus
[Reaction:R-MMU-9652264] ERBB2 binds TKIs - Mus musculus
output
[Complex:R-HSA-9665220] ERBB2:TKIs:ERBIN:HSP90:CDC37 [plasma membrane]
releaseDate
2019-12-10
reviewStatus
[ReviewStatus:9821382] five stars
reviewed
[InstanceEdit:9662685] Kancha, Rama Krishna, 2019-09-16
schemaClass
Reaction
species
[Species:48887] Homo sapiens
stId
R-HSA-9652264
summation
[Summation:9652249] ERBB2 can bind to and be inhibited by the following tyrosine...
Referrals
(hasEvent)
[Pathway:R-HSA-9634285] Constitutive Signaling by Overexpressed ERBB2
[Pathway:R-HSA-9652282] Drug-mediated inhibition of ERBB2 signaling
(normalReaction)
[FailedReaction:R-HSA-9665304] ERBB2 T862A does not bind sapitinib
[FailedReaction:R-HSA-9665315] ERBB2 T733I does not bind tesevatinib
[FailedReaction:R-HSA-9665286] Resistant ERBB2 KD mutants do not bind neratinib
[FailedReaction:R-HSA-9665280] ERBB2 KD mutants do not bind osimertinib
[FailedReaction:R-HSA-9665311] ERBB2 T798M does not bind afatinib
[FailedReaction:R-HSA-9665278] Resistant ERBB2 KD mutants do not bind AEE788
[FailedReaction:R-HSA-9665284] Resistant ERBB2 KD mutants do not bind lapatinib
[Reaction:R-HSA-9665412] ERBB2 ECD mutants bind TKIs
[Reaction:R-HSA-9665702] ERBB2 TMD/JMD mutants bind TKIs
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