Imatinib-resistant PDGFR mutants

Stable Identifier
R-HSA-9674396
Type
Pathway
Species
Homo sapiens
ReviewStatus
5/5
Locations in the PathwayBrowser
Expand all
General
SVG | 
PNG
Low
Medium
High
 | PPTX  | SBGN
Imatinib-resistant PDGFR mutants
Click the image above or here to open this pathway in the Pathway Browser
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
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
Participants
Events
Participates
as an event of
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)
Cite Us!