Platelet-derived growth factor receptor kinase

Fig. 2. Presentation of the intracellular domain of the PDGF (platelet-derived growth factor) receptor. The two catalytically active kinase domains are highlighted. Docking sites for SH2 domains are symbolized with a pTyr sidechain. SH2 domains identified to bind to the corresponding phosphorylated tyrosines (numbered on the left) are schematically depicted and labeled on the right...

Miyake, S., M. L. Lupher, Jr., B. Druker, and H. Band. The tyrosine kinase regulator Cbl enhances the ubiquitination and degradation of the platelet-derived growth factor receptor alpha. Proc Natl Acad Sci USA. 95 7927-7932.1998. 

Miyake, S., K. P. Mullane-Robinson, N. L. Lill, P. Douillard, and H. Band. Cbl-mediated negative regulation of platelet-derived growth factor receptor-dependent cell proliferation. A critical role for Cbl tyrosine kinase-binding domain. J Biol Chem. 274 16619-28.1999. 

Hu P, Margolis B, Skolnik EY et al. Interaction of phosphatidylinositol 3-kinase-associated p85 with epidermal growth factor and platelet-derived growth factor receptors. Mo/ Cell Biol 1992 12 981-990. Li N, Batzer A, Daly R et al. Guanine-nucleotide-releasing factor hSosl binds to Grb2 and links receptor tyrosine kinases to Ras signalling. Nature 1993 363 85-88. 

Domin, J. Dhand, R. Waterfield, M.D. Binding to the platelet-derived growth factor receptor transiently activates the p85a-pll0a phosphoinositide 3-kinase complex in vivo. J. Biol. Chem., 271, 21614-21621 (1996)... 

PDGFR.platelet-derived growth factor receptor, a kinase... 

Imatinib (STI571) is an inhibitor of the tyrosine kinase domain of the Bcr-Abl oncoprotein and prevents the phosphorylation of the kinase substrate by ATP. It is indicated for the treatment of chronic myelogenous leukemia (CML), a pluripotent hematopoietic stem cell disorder characterized by the t(9 22) Philadelphia chromosomal translocation. This translocation results in the Bcr-Abl fusion protein, the causative agent in CML, and is present in up to 95% of patients with this disease. This agent inhibits other activated receptor tyrosine kinases for platelet-derived growth factor receptor (PDGFR), stem cell factor (SCF), and c-kit. 

Mendel DB et al (2003) In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res 9 327-337... 

Mondorf UF, Geiger H, Herrero M, Zeuzem S, Piiper A. 2000. Involvement of the platelet-derived growth factor receptor in angiotensin Il-induced activation of extracellular regulated kinases 1 and 2 in human mesangial cells 1. FEBS Lett 472 129-132. 

PDGF, platelet-derived growth factor PDGF-RTK, platelet-derived growth factor receptor tyrosine kinase PDPK, phosphatidylinositol lipid-dependent PK... 

Park CS, Schneider IC, Haugh JM. Kinetic analysis of platelet-derived growth factor receptor/phosphoinositide 3-kinase/Akt signaling in fibroblasts. J. Biol. Chem. 2003 278 37064-37072. 

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