化学
拟肽
细胞外
表皮生长因子受体
表皮生长因子受体抑制剂
信号转导
磷酸化
体内
表皮生长因子
肽
小分子
生物化学
受体
癌症研究
体外
细胞生物学
生物
生物技术
作者
Mengmeng Zheng,Chunpu Li,Mi Zhou,Ru Jia,Gang Cai,Fengyu She,Lulu Wei,Shaohui Wang,Jie Yu,Dingyan Wang,Laurent Calcul,Xingmin Sun,Xiaomin Luo,Feng Cheng,Qi Li,Yan Wang,Jianfeng Cai
标识
DOI:10.1021/acs.jmedchem.1c00607
摘要
It is very promising to target the extracellular domain of epidermal growth factor receptor (EGFR) for developing novel and selective anticancer therapies. Herein, we report the discovery of a novel small molecule, M-2-5, from a one-bead-two-compound (OBTC) cyclic γ-AApeptide library. The molecule was found to bind tightly to the extracellular domain of EGFR. Intriguingly, this molecule could also effectively antagonize EGF-stimulated EGFR phosphorylation and downstream signal transduction. Furthermore, together with its remarkable resistance to proteolytic degradation, M-2-5 was shown to effectively inhibit cell proliferation and migration in vitro and suppresses the growth of tumor in the A549 xenograft model in vivo, highlighting its potential therapeutic application for cancer treatment.
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