Literature summary for 2.7.10.1 extracted from

Wilhelm, S.M.; Adnane, L.; Newell, P.; Villanueva, A.; Llovet, J.M.; Lynch, M.
Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling (2008), Mol. Cancer Ther., 7, 3129-3140.

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Application

Application	Comment	Organism
drug development	sorafenib, a multikinase inhibitor of both Raf and VEGF and PDGF receptor tyrosine kinase signaling, inhibits tumor growth and disrupts tumor microvasculature through antiproliferative, antiangiogenic, and/or proapoptotic effects, suggesting its broad preclinical and clinical activity. The inhibitor shows antitumor activity in phase II/III trials involving patients with advanced renal cell carcinoma and hepatocellular carcinoma	Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
T670I	cKit mutant, that renders patients with gastrointestinal stromal tumor refractory to imatinib	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
siRNA	blocks VEGF secretion by melanoma tumors	Homo sapiens
sorafenib	oral multikinase inhibitor, inhibits receptor tyrosine kinase autophosphorylation, implicated in tumorigenesis and tumor progression	Homo sapiens
sorafenib	oral multikinase inhibitor, inhibits receptor tyrosine kinase autophosphorylation	Mus musculus
sunitinib	VEGFR tyrosine kinase inhibitor	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Mus musculus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
EoL-1 cell	expresses Flt-3	Homo sapiens	-
additional information	MV4-11 cell expresses Flt-3. HAoSMC cell expresses PDGFR-beta. RS4-11 cell expresses Flt-1. Present in RCC786-O cell and UACC 903 cell. Overexpression of VEGFR mRNA in HCC cell	Homo sapiens	-
additional information	RenCa cell	Mus musculus	-
NIH-3T3 cell	expresses VEGFR-2	Mus musculus	-

Synonyms

Synonyms	Comment	Organism
cKit	-	Homo sapiens
Flt-1	-	Homo sapiens
FLT-3	-	Homo sapiens
PDGF receptor tyrosine kinase	-	Mus musculus
PDGF receptor tyrosine kinase	-	Homo sapiens
PDGFR-beta	-	Mus musculus
PDGFR-beta	-	Homo sapiens
platelet-derived growth factor receptor	-	Mus musculus
platelet-derived growth factor receptor	-	Homo sapiens
RET	-	Homo sapiens
vascular endothelial growth factor receptor	-	Mus musculus
vascular endothelial growth factor receptor	-	Homo sapiens
VEGF receptor tyrosine kinase	-	Mus musculus
VEGF receptor tyrosine kinase	-	Homo sapiens
VEGFR tyrosine kinase	-	Homo sapiens
VEGFR-1	-	Homo sapiens
VEGFR-2	-	Homo sapiens
VEGFR-3	-	Homo sapiens

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Release 2023.1 (January 2023)