D842V PDGFRA doesn't bind sunitinib

Stable Identifier
R-HSA-9674398
Type
Reaction [transition]
Species
Homo sapiens
Compartment
plasma membrane, cytosol
ReviewStatus
5/5
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D842V PDGFRA doesn't bind sunitinib
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Sunitinib-resistant PDFGRA mutants include the D842V allele, occuring in the activation loop of the receptor, and the Y288C allele, which occurs in the extracellular domain and results in a version of the receptor that signals from intracellular compartments (Heinrich et al, 2008; Heinrich et al, 2012; Ip et al, 2019). Only the resistance of the D842V mutant is shown in this failed reaction.
Literature References
PubMed ID Title Journal Year
30389923 Neomorphic PDGFRA extracellular domain driver mutations are resistant to PDGFRA targeted therapies

Ip, CKM, Ng, PKS, Jeong, KJ, Shao, SH, Ju, Z, Leonard, PG, Hua, X, Vellano, CP, Woessner, R, Sahni, N, Scott, KL, Mills, GB

Nat Commun 2018
22665524 Sorafenib inhibits many kinase mutations associated with drug-resistant gastrointestinal stromal tumors

Heinrich, MC, Mariño-Enríquez, A, Presnell, A, Donsky, RS, Griffith, DJ, McKinley, A, Patterson, J, Taguchi, T, Liang, CW, Fletcher, JA

Mol. Cancer Ther. 2012
18955458 Primary and secondary kinase genotypes correlate with the biological and clinical activity of sunitinib in imatinib-resistant gastrointestinal stromal tumor

Heinrich, MC, Maki, RG, Corless, CL, Antonescu, CR, Harlow, A, Griffith, D, Town, A, McKinley, A, Ou, WB, Fletcher, JA, Fletcher, CD, Huang, X, Cohen, DP, Baum, CM, Demetri, GD

J. Clin. Oncol. 2008
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as an event of
Normal reaction
PDGFRs bind type II TKI (Homo sapiens)
Functional status

Loss of function of PDGFRA D842V [plasma membrane]

Normal Entity
Disease Entity
Status
Disease
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
Cross References
Mondo
Authored
Rothfels, K  (2020-02-25)
Reviewed
Ip, CKM  (2020-02-06)
Created
Rothfels, K  (2020-01-13)
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