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Details on Person ERBB2 binds TKIs

Class:IdReaction:9652264
_displayNameERBB2 binds TKIs
_doReleaseTRUE
_timestamp2024-03-20 23:46:13
authored[InstanceEdit:9656339] Orlic-Milacic, Marija, 2019-07-31
compartment[Compartment:70101] cytosol
[Compartment:876] plasma membrane
created[InstanceEdit:9652267] Orlic-Milacic, Marija, 2019-06-28
edited[InstanceEdit:9665760] Orlic-Milacic, Marija, 2019-11-01
input[Complex:1227970] ERBB2:ERBIN:HSP90:CDC37 [plasma membrane] [Homo sapiens]
[DefinedSet:9652360] lapatinib, neratinib, afatinib, AZ5104, tesevatinib, canertinib, sapitinib, CP-724714, AEE78 [cytosol]
isChimericFALSE
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 HER2T798I 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
modified[InstanceEdit:9652345] Orlic-Milacic, Marija, 2019-06-28
[InstanceEdit:9652372] Orlic-Milacic, Marija, 2019-06-28
[InstanceEdit:9665224] Orlic-Milacic, Marija, 2019-10-30
[InstanceEdit:9665326] Orlic-Milacic, Marija, 2019-10-30
[InstanceEdit:9666033] Orlic-Milacic, Marija, 2019-11-01
[InstanceEdit:9666039] Orlic-Milacic, Marija, 2019-11-01
[InstanceEdit:9666040] Orlic-Milacic, Marija, 2019-11-01
[InstanceEdit:9666041] Orlic-Milacic, Marija, 2019-11-01
[InstanceEdit:9666042] Orlic-Milacic, Marija, 2019-11-01
[InstanceEdit:9666684] Orlic-Milacic, Marija, 2019-11-05
[InstanceEdit:9667205] Orlic-Milacic, Marija, 2019-11-08
[InstanceEdit:9667512] Orlic-Milacic, Marija, 2019-11-12
[InstanceEdit:9830342] Matthews, Lisa, 2023-03-08
[InstanceEdit:9866055] Orlic-Milacic, Marija, 2024-03-20
nameERBB2 binds TKIs
output[Complex:9665220] ERBB2:TKIs:ERBIN:HSP90:CDC37 [plasma membrane] [Homo sapiens]
precedingEvent
releaseDate2019-12-10
reviewed[InstanceEdit:9662685] Kancha, Rama Krishna, 2019-09-16
reviewStatus[ReviewStatus:9821382] five stars
species[Species:48887] Homo sapiens
stableIdentifier[StableIdentifier:9652291] R-HSA-9652264.3
summation[Summation:9652249] ERBB2 can bind to and be inhibited by the following tyrosine...
(hasEvent)[Pathway:9634285] Constitutive Signaling by Overexpressed ERBB2 [Homo sapiens]
[Pathway:9652282] Drug-mediated inhibition of ERBB2 signaling [Homo sapiens]
(normalReaction)[FailedReaction:9650096] ERBB2 L755S does not bind TKIs [Homo sapiens]
[FailedReaction:9650278] ERBB2 V777L does not bind AEE788 [Homo sapiens]
[FailedReaction:9650938] ERBB2 V842I does not bind lapatinib [Homo sapiens]
[FailedReaction:9665278] Resistant ERBB2 KD mutants do not bind AEE788 [Homo sapiens]
[FailedReaction:9665280] ERBB2 KD mutants do not bind osimertinib [Homo sapiens]
[FailedReaction:9665284] Resistant ERBB2 KD mutants do not bind lapatinib [Homo sapiens]
[FailedReaction:9665286] Resistant ERBB2 KD mutants do not bind neratinib [Homo sapiens]
[FailedReaction:9665304] ERBB2 T862A does not bind sapitinib [Homo sapiens]
[FailedReaction:9665311] ERBB2 T798M does not bind afatinib [Homo sapiens]
[FailedReaction:9665315] ERBB2 T733I does not bind tesevatinib [Homo sapiens]
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