In this study, we aimed to determine VEGFR-2, EGFR and PDGFR-β tyrosine kinase inhibitory activities of some pyrrolo[2,3-d]pyrimidine derivatives previously synthesized and showed potent cytotoxic and apoptotic effects against several cancer cell lines by our group and to evaluate the relationships between inhibitory activities and binding properties of the active compounds by molecular docking...

OBJECTIVE Somatic mutations in the epidermal growth factor receptor gene are associated with a therapeutic response to epidermal growth factor receptor tyrosine kinase inhibitors such as gefitinib and erlotinib in patients with non-small cell lung cancer. Although the safety profile of these drugs is favorable, a small proportion of patients with EGFR mutation-positive non-small cell lung cance...

It has previously been demonstrated that the insulin-mimetic agent trypsin stimulates autophosphorylation of purified insulin receptors and activates the insulin receptor tyrosine kinase in vitro. We now report the effects of trypsin on whole cell tyrosine kinase activation and insulin receptor autophosphorylation. Trypsin treatment of intact adipocytes produces a time-dependent stimulation of ...

Mutation of the epidermal growth factor receptor (EGF-R) within the ATP binding subdomain results in a receptor that lacks tyrosine kinase activity and is defective in signal transduction. However, this kinase-negative EGF-R is able to activate MAP kinase (Campos-Gonzalez, R., and Glenny, J. R. (1992) J. Biol. Chem. 267, 14535-14538). This observation suggests that signal initiation by the EGF-...

Many developmental processes are regulated by intercellular signaling mechanisms that employ the activation of receptor tyrosine kinases. One model system that has been particular useful in determining the role of receptor tyrosine kinase-mediated signaling processes in cell fate determination is the developing Drosophila eye. The specification of the R7 photoreceptor cell in each ommatidium of...

The epidermal growth factor (EGF) receptor has been shown to posses an intrinsic tyrosine protein kinase activity that is stimulated by the binding ofEGF [1]. In addition, two other ligands for the EGF receptor can stimulate the tyrosine protein kinase activity in intact cells: TGF-(X (transforming growth factor (X) and a soluble biosynthetic precursor of TGF-(X [2, 3]. Analysis of the kinetics...

Insulin binding and tyrosine kinase activity of the insulin receptor have been measured in the liver and muscles of rats fed or submitted to a 72-h-fasting. In both tissues, insulin binding increased in fasting rats. In liver, the ability of insulin to simulate receptor tyrosine kinase activity greatly unpaired during fasting, but remained unchanged in muscle. The change during fasting of the i...