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Raf dimer inhibitors bind RAF heterodimers
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authored
[InstanceEdit:9664643] Rothfels, Karen, 2019年10月25日
category
binding
compartment
[Compartment:876] plasma membrane
[Compartment:70101] cytosol
created
[InstanceEdit:9653110] Rothfels, Karen, 2019年07月09日
dbId
9653108
displayName
Raf dimer inhibitors bind RAF heterodimers
edited
[InstanceEdit:9690121] Rothfels, Karen, 2020年05月26日
eventOf
[Pathway:R-HSA-5673000] RAF activation - Homo sapiens
input
[Complex:R-HSA-5672733] p21 RAS:GTP:homo/heterodimerized RAF complex [plasma membrane]
[DefinedSet:R-ALL-9657579] RAF dimer inhibitors [cytosol]
isChimeric
false
isInDisease
false
isInferred
false
literatureReference
[LiteratureReference:9652955] Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers
[LiteratureReference:9657209] Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma
[LiteratureReference:9657180] A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas
[LiteratureReference:9652925] LY3009120, a panRAF inhibitor, has significant anti-tumor activity in BRAF and KRAS mutant preclinical models of colorectal cancer
[LiteratureReference:9652971] Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells
[LiteratureReference:9657340] Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives
[LiteratureReference:9686653] New perspectives for targeting RAF kinase in human cancer
[LiteratureReference:9686649] Current Insights of BRAF Inhibitors in Cancer
maxDepth
1
modified
[InstanceEdit:11064438] Weiser, Joel, 2025年08月28日
name
Raf dimer inhibitors bind RAF heterodimers
orthologousEvent
[Reaction:R-PFA-9653108] Raf dimer inhibitors bind RAF heterodimers - Plasmodium falciparum
[Reaction:R-CEL-9653108] Raf dimer inhibitors bind RAF heterodimers - Caenorhabditis elegans
[Reaction:R-DME-9653108] Raf dimer inhibitors bind RAF heterodimers - Drosophila melanogaster
[Reaction:R-GGA-9653108] Raf dimer inhibitors bind RAF heterodimers - Gallus gallus
[Reaction:R-SSC-9653108] Raf dimer inhibitors bind RAF heterodimers - Sus scrofa
[Reaction:R-BTA-9653108] Raf dimer inhibitors bind RAF heterodimers - Bos taurus
[Reaction:R-CFA-9653108] Raf dimer inhibitors bind RAF heterodimers - Canis familiaris
[Reaction:R-RNO-9653108] Raf dimer inhibitors bind RAF heterodimers - Rattus norvegicus
[Reaction:R-MMU-9653108] Raf dimer inhibitors bind RAF heterodimers - Mus musculus
output
[Complex:R-HSA-9653109] p21RAS:GTP:homo/heterodimerized RAF complex:RAF dimer inhibitors [plasma membrane]
precedingEvent
[Reaction:R-HSA-5672966] RAS:GTP:'activator' RAF homo/heterodimerizes with other RAF monomers - Homo sapiens
releaseDate
2020年06月10日
reviewStatus
[ReviewStatus:9821382] five stars
reviewed
[InstanceEdit:9686656] Gavathiotis, Evripidis, 2020年05月04日
schemaClass
Reaction
species
[Species:48887] Homo sapiens
stId
R-HSA-9653108
summation
[Summation:9653037] LY3009120, TAK-580 and TAK-632 are pan-RAF inhibitors that b...
Referrals
(hasEvent)
[Pathway:R-HSA-5673000] RAF activation
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