Autophosphorylation of PDGFR mutant dimers

Stable Identifier
R-HSA-9672175
Type
Reaction [transition]
Species
Homo sapiens
Compartment
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Activating mutations in the kinase, juxtamembrane and transmembrane domains of PDGFRA lead to constitutive, ligand-independent dimerization and trans-autophosphorylation, and stimulate downstream signaling pathways (Heinrich et al, 2003; Hirota et al, 2003; Corless et al, 2005; Velghe et al, 2014; reviewed in Roskoski et al, 2018; Klug et al, 2018).

Literature References
PubMed ID Title Journal Year
12522257 PDGFRA activating mutations in gastrointestinal stromal tumors

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

Science 2003
29408302 The role of small molecule platelet-derived growth factor receptor (PDGFR) inhibitors in the treatment of neoplastic disorders

Roskoski, R

Pharmacol. Res. 2018
12949711 Gain-of-function mutations of platelet-derived growth factor receptor alpha gene in gastrointestinal stromal tumors

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

Gastroenterology 2003
29964125 Structural and clinical consequences of activation loop mutations in class III receptor tyrosine kinases

Klug, LR, Kent, JD, Heinrich, MC

Pharmacol. Ther. 2018
15928335 PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib

Corless, CL, Schroeder, A, Griffith, D, Town, A, McGreevey, L, Harrell, P, Shiraga, S, Bainbridge, T, Morich, J, Heinrich, MC

J. Clin. Oncol. 2005
23752188 PDGFRA alterations in cancer: characterization of a gain-of-function V536E transmembrane mutant as well as loss-of-function and passenger mutations

Velghe, AI, Van Cauwenberghe, S, Polyansky, AA, Chand, D, Montano-Almendras, CP, Charni, S, Hallberg, B, Essaghir, A, Demoulin, JB

Oncogene 2014
Participants
Participant Of
Catalyst Activity
Catalyst Activity
Title
protein tyrosine kinase activity of PDGFR mutant dimers [plasma membrane]
Physical Entity
Activity
Normal reaction
Disease
Name Identifier Synonyms
cancer 162 malignant tumor, malignant neoplasm, primary cancer
Authored
Reviewed
Created
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