PI3-kinase binds to mutant PDGFR receptor

Stable Identifier
R-HSA-9672172
Type
Reaction [binding]
Species
Homo sapiens
Compartment
cytosol, plasma membrane
ReviewStatus
5/5
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PI3-kinase binds to mutant PDGFR receptor
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Gain-of-function mutants of PDGFRA bind to phosphatidylinositol-3' kinase (PI3K) to activate AKT signaling, as assessed by the presence of phosphorylated AKT in Western blot analysis (Heinrich et al, 2003; Ohashi et al, 2004; reviewed in Corless et al, 2011). Interaction of PI3K with mutant PDGFRA receptors is assumed to occur through binding to phosphorylated Y731 and Y742 as is the case for the wild-type receptor, although this hasn't been directly demonstrated (reviewed in Roskoski, 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
15221957 Different inhibitory effect of imatinib on phosphorylation of mitogen-activated protein kinase and Akt and on proliferation in cells expressing different types of mutant platelet-derived growth factor receptor-alpha

Kitamura, Y, Shinomura, Y, Isozaki, K, Nishida, T, Kinoshita, K, Ohashi, A, Hirota, S

Int. J. Cancer 2004
12522257 PDGFRA activating mutations in gastrointestinal stromal tumors

Corless, CL, Heinrich, MC, Singer, S, Griffith, DJ, Town, A, Haley, A, Duensing, A, McGreevey, L, Fletcher, JA, Demetri, GD, Joseph, N, Chen, CJ, Fletcher, CD

Science 2003
Participants
Input
Output
Participates
as an event of
Normal reaction
PI3-kinase binds to the active receptor (Homo sapiens)
Functional status

Gain of function of p-11Y PDGFR mutant receptor dimers [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  (2019-12-23)
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