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Sunitinib-resistant PDGFR mutants
Stable Identifier
R-HSA-9674401
Type
Pathway
Species
Homo sapiens
ReviewStatus
5/5
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Disease (Homo sapiens)
Diseases of signal transduction by growth factor receptors and second messengers (Homo sapiens)
Signaling by PDGFR in disease (Homo sapiens)
Drug resistance of PDGFR mutants (Homo sapiens)
Sunitinib-resistant PDGFR mutants (Homo sapiens)
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Sunitinib is a class II TKI that is often used as a second-line treatment in PDGFR- and KIT-driven cancers that develop resistance to imatinib (reviewed in Corless et al, 2011; Klug et al, 2018). Sunintib is approved for the treatment of renal cell carcinoma, GIST and pancreatic tumors. A number of PDGFR mutations exhibit resistance to inhibition by sunitinib (Roskoski, 2007; reviewed in Roskoski, 2018; Klug et al, 2018).
Literature References
PubMed ID
Title
Journal
Year
22089421
Gastrointestinal stromal tumours: origin and molecular oncology
Barnett, CM
,
Corless, CL
,
Heinrich, MC
Nat. Rev. Cancer
2011
29408302
The role of small molecule platelet-derived growth factor receptor (PDGFR) inhibitors in the treatment of neoplastic disorders
Roskoski, R
Pharmacol. Res.
2018
29964125
Structural and clinical consequences of activation loop mutations in class III receptor tyrosine kinases
Heinrich, MC
,
Kent, JD
,
Klug, LR
Pharmacol. Ther.
2018
17367763
Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor
Roskoski, R
Biochem. Biophys. Res. Commun.
2007
Participants
Events
D842V PDGFRA doesn't bind sunitinib
(Homo sapiens)
Participates
as an event of
Drug resistance of PDGFR mutants (Homo sapiens)
Disease
Name
Identifier
Synonyms
cancer
DOID:162
malignant tumor, malignant neoplasm, primary cancer
Authored
Rothfels, K (2020-02-25)
Reviewed
Ip, CKM (2020-02-06)
Created
Rothfels, K (2020-01-13)
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