Sunitinib-resistant PDGFR mutants

Stable Identifier
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
29408302 The role of small molecule platelet-derived growth factor receptor (PDGFR) inhibitors in the treatment of neoplastic disorders

Roskoski, R

Pharmacol. Res. 2018
22089421 Gastrointestinal stromal tumours: origin and molecular oncology

Corless, CL, Barnett, CM, Heinrich, MC

Nat. Rev. Cancer 2011
29964125 Structural and clinical consequences of activation loop mutations in class III receptor tyrosine kinases

Klug, LR, Kent, JD, Heinrich, MC

Pharmacol. Ther. 2018
17367763 Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor

Roskoski, R

Biochem. Biophys. Res. Commun. 2007
Participant Of
Name Identifier Synonyms
cancer 162 malignant tumor, malignant neoplasm, primary cancer
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