Imatinib-resistant PDGFR mutants

Stable Identifier
R-HSA-9674396
Type
Pathway
Species
Homo sapiens
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A number of PDGFRA mutations found in GIST and other cancers are resistant to inhibition with imatinib (reviewed in Corless et al, 2011). These include the most common allele D842V, which occurs in the activation loop of the receptor, as well as S601P and the gatekeeper mutation T674I (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
Participants
Participant Of
Disease
Name Identifier Synonyms
cancer 162 malignant tumor, malignant neoplasm, primary cancer
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