Pharmacoproteomic study of the effects of different concentrations of Sunitinib, a multi-targeted receptor tyrosine kinase inhibitor, using triple SILAC

摘要

Receptor tyrosine kinases (RTKs) are a subclass of transmembrane-spanning receptors with intrinsic ligand-inducible protein tyrosine kinase activity. In humans deregulation of RTKs causes cellular transformation and has been demonstrated to play a significant role in oncogenesis. Inhibition of RTKs by small molecule drugs has evolved into a major therapeutic strategy. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor. However, the mechanism of its action including formation of resistance is not fully elucidated. The investigation of the actions of this small molecule inhibitor on cellular machinery is of particular interest, as a more detailed understanding of its effects could have profound implications for the identification of novel tractable targets as well as providing greater insights into the signaling mechanisms at play within RTK pathways.