Sorafenib-resistant PDGFR mutants don't bind sorefenib

Stable Identifier
R-HSA-9674414
Type
Reaction [transition]
Species
Homo sapiens
Compartment
plasma membrane, cytosol
ReviewStatus
5/5
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Sorafenib-resistant PDGFR mutants don't bind sorefenib
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Sorafenib has broader effectiveness against many imatinib-resistant PDGFR mutations that sunitinib, however both D842V and S601P show resistance to inhibition by sorafenib as well (Heinrich et al, 2012; Salemi et al, 2009; reviewed in Corless et al, 2011).
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
19210352 A novel FIP1L1-PDGFRA mutant destabilizing the inactive conformation of the kinase domain in chronic eosinophilic leukemia/hypereosinophilic syndrome

Scapozza, L, Simon, D, Salemi, S, Moretti, L, Simon, HU, Yousefi, S, Schmid, I

Allergy 2009
22665524 Sorafenib inhibits many kinase mutations associated with drug-resistant gastrointestinal stromal tumors

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

Mol. Cancer Ther. 2012
Participants
Input
Participates
as an event of
Normal reaction
PDGFRs bind type II TKI (Homo sapiens)
Functional status

Loss of function of sorafenib-resistant PDGFR mutants [plasma membrane]

Normal Entity
Disease Entity
Status
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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