Platelet-derived growth factor inhibitors

Platelet-activating Factor Platelet Aggregation Inhibitors Platelet-derived Growth Factor Receptor Platelet Inhibitors Platelets... 

Fujio Y, Yamada F, Takahashi K, Shibata N. Responses of smooth muscle cells to platelet-derived growth factor are inhibited by herbimycin-A tyrosine kinase inhibitor. Biochem Biophys Res Commun 1993 195(1) 79—83. 

Katritzky, A.R. et al., QSAR studies in 1-phenylbenzimidazoles as inhibitors of the platelet-derived growth factor, Bioorg. Med. Chem., 13,6598,2005. 

Imatinib is an inhibitor of the protein tyrosine kinase involved with platelet-derived growth factor (Bcr-ABL). A loss of cellular control of this tyrosine kinase has been identified as a key mechanism for malignant cell growth. The ability of imatinib to inhibit Bcr-ABL provides a rationale for its use in the treatment of human cancers such as Philadelphia... 

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. 

Platelet aggregation different pathways of activation. Abbreviations ADR adenosine diphosphate ATP, adenosine triphosphate COX, cyclooxygenase PAI, plasminogen activator inhibitor PDGF, platelet derived growth factor. 

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... 

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