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Discovery of Cyclic Peptidomimetic Ligands Targeting the Extracellular Domain of EGFR

文献类型：期刊论文

作者Zheng, Mengmeng1; Li, Chunpu1,2,3; Zhou, Mi1; Jia, Ru2,3; Cai, Gang2,3; She, Fengyu1; Wei, Lulu1; Wang, Shaohui4; Yu, Jie5; Wang, Dingyan5
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2021-08-12
卷号64期号:15页码:11219-11228
ISSN号0022-2623
DOI10.1021/acs.jmedchem.1c00607
通讯作者Li, Qi(qili@shutcm.edu.cn) ; Wang, Yan(yanwang@shutcm.edu.cn) ; Cai, Jianfeng(Jianfengcai@usf.edu)
英文摘要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 gamma-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.
WOS关键词EPIDERMAL-GROWTH-FACTOR ; FACTOR RECEPTOR ; SIGNAL-TRANSDUCTION ; GAMMA-AAPEPTIDES ; PEPTIDE LIGAND ; CANCER ; BINDING ; MUTATIONS ; GEFITINIB ; THERAPY
资助项目USF ; National Natural Science Foundation of China[81520108031] ; National Natural Science Foundation of China[81573764] ; National Natural Science Foundation of China[81774095] ; Municipal Human Resources Development Program for Outstanding Leaders in Medical Disciplines in Shanghai[2017BR031] ; Threeyear Plan for the Development of TCM[ZY (2018-2020). CCCX-2003-03]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000685644300039
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/297648]  
专题中国科学院上海药物研究所
通讯作者Li, Qi; Wang, Yan; Cai, Jianfeng
作者单位1.Univ S Florida, Dept Chem, Tampa, FL 33620 USA
2.Shanghai Univ Tradit Chinese Med, Shuguang Hosp, Dept Med Oncol, Shanghai 201203, Peoples R China
3.Shanghai Univ Tradit Chinese Med, Shuguang Hosp, Canc Inst Med, Shanghai 201203, Peoples R China
4.Univ S Florida, Morsani Coll Med, Dept Mol Med, Tampa, FL 33612 USA
5.Chinese Acad Sci, Drug Discovery & Design Ctr, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
6.Univ S Florida, Coll Pharm, Dept Pharmaceut Sci, Tampa, FL 33612 USA
7.Shanghai Univ Tradit Chinese Med, Acad Integrat Med, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Zheng, Mengmeng,Li, Chunpu,Zhou, Mi,et al. Discovery of Cyclic Peptidomimetic Ligands Targeting the Extracellular Domain of EGFR[J]. JOURNAL OF MEDICINAL CHEMISTRY,2021,64(15):11219-11228.
APA Zheng, Mengmeng.,Li, Chunpu.,Zhou, Mi.,Jia, Ru.,Cai, Gang.,...&Cai, Jianfeng.(2021).Discovery of Cyclic Peptidomimetic Ligands Targeting the Extracellular Domain of EGFR.JOURNAL OF MEDICINAL CHEMISTRY,64(15),11219-11228.
MLA Zheng, Mengmeng,et al."Discovery of Cyclic Peptidomimetic Ligands Targeting the Extracellular Domain of EGFR".JOURNAL OF MEDICINAL CHEMISTRY 64.15(2021):11219-11228.

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来源：上海药物研究所

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