Erkitinib, a novel EGFR tyrosine kinase inhibitor screened using a ProteoChip system from a phytochemical library.
作者： Eung-Yoon Kim , Young-Jin Choi , Chan-Won Park , In-Cheol Kang
DOI: 10.1016/J.BBRC.2009.08.141
关键词:
摘要: Receptor tyrosine kinases (PTKs) play key roles in the pathogenesis of numerous human diseases, including cancer. Therefore PTK inhibitors are currently under intensive investigation as potential drug candidates. Herein, we report on a ProteoChip-based screening an epidermal growth factor receptor (EGFR) kinase (TK) inhibitor, Erkitinibs, from phytochemical libraries. PLC-γ-1 was used substrate immobilized ProteoChip and incubated with EGFR to phosphorylate residues substrate, followed by fluorescence detection recognized phospho-specific monoclonal antibody. Erkitinibs inhibited HeLa cell proliferation dose-dependent manner. In conclusion, these data suggest that can be specific inhibitor further developed potent anti-tumor agent.
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