Blocking of EGF-Dependent Cell Proliferation by EGF Receptor Kinase Inhibitors
作者： P. Yaish , A. Gazit , C. Gilon , A. Levitzki
关键词: Tropomyosin receptor kinase C 、 Tyrosine kinase 、 Platelet-derived growth factor receptor 、 Cyclin-dependent kinase 9 、 Biology 、 MAP kinase kinase kinase 、 Receptor tyrosine kinase 、 Kinase activity 、 Mitogen-activated protein kinase kinase 、 Molecular biology
摘要: A systematic series of low molecular weight protein tyrosine kinase inhibitors were synthesized; they had progressively increasing affinity over a 2500-fold range toward the substrate site epidermal growth factor (EGF) receptor domain. These compounds inhibited EGF activity up to three orders magnitude more than insulin kinase, and also effectively EGF-dependent autophosphorylation receptor. The most potent proliferation A431/clone 15 cells with little or no effect on EGF-independent these cells. potential use as antiproliferative agents is demonstrated.
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