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	Targeted peptide-au cluster binds to epidermal growth factor receptor (egfr) in both active and inactive states: a clue for cancer inhibition through dual pathways
	Zhang, Peng1,2; Zhai, Jiao2; Gao, Xueyun3; Zhao, Hongkang1; Su, Wenyong1; Zhao, Lina2
刊名	Science bulletin
	2018-03-30
卷号	63期号:6页码:349-355
关键词	Peptide-au cluster Egfr Targeted binding Anticancer
ISSN号	2095-9273
DOI	10.1016/j.scib.2018.02.007
通讯作者	Zhao, lina(linazhao@ihep.ac.cn)
英文摘要	The epidermal growth factor receptor (egfr) has become an important target protein in anticancer drug development. meanwhile, peptide-au cluster has been proposed as potential targeted nano-drug assembled by targeting peptide. here, we designed and synthesized a novel peptide-au cluster as au(10)peptide(5) to target to egfr. we found au(10)peptide(5) could target to the natural binding sites of all egfrs at membrane in both active and inactive states by molecular simulations. its targeted ability was further verified by the co-localization and blocking experiments. we also study the configuration modifications of both active and inactive egfrs after binding by au(10)peptide(5). for active egfr, the absorbed au(10)peptide(5) might replace the natural ligand in egfr endocytosis process. then, the peptide-au cluster in endochylema could inhibit the cancer relating enzyme activity including thioredoxin reductase1 (trxr1) and induce the oxidative stress mediated apoptosis in tumor cells. for inactive egfr, it was retained in inactive state by au(10)peptide(5) binding to inhibit dimerization of egfr for anticancer. both pathways might be applied in anticancer drug development based on the theoretical and experimental study here. (c) 2018 science china press. published by elsevier b.v. and science china press. all rights reserved.
WOS关键词	THIOREDOXIN REDUCTASE 1 ; ALPHA(IIB)BETA(3) INTEGRIN ; BREAST-CANCER ; TUMOR ; CELLS ; NANOCLUSTERS ; THERAPY ; NANOPARTICLES ; RADIOTHERAPY ; COMPLEXES
WOS研究方向	Science & Technology - Other Topics
WOS类目	Multidisciplinary Sciences
语种	英语
出版者	SCIENCE PRESS
WOS记录号	WOS:000429784000006
内容类型	期刊论文
URI标识	http://www.corc.org.cn/handle/1471x/2178186
专题	高能物理研究所
通讯作者	Zhao, Lina
作者单位	1.Beijing Inst Technol, Sch Phys, Beijing 100081, Peoples R China 2.Chinese Acad Sci, Inst High Energy Phys, Key Lab Biomed Effects Nanomat & Nanosafety, Beijing 100049, Peoples R China 3.Beijing Univ Technol, Dept Chem & Chem Engn, Beijing 100049, Peoples R China
推荐引用方式 GB/T 7714	Zhang, Peng,Zhai, Jiao,Gao, Xueyun,et al. Targeted peptide-au cluster binds to epidermal growth factor receptor (egfr) in both active and inactive states: a clue for cancer inhibition through dual pathways[J]. Science bulletin,2018,63(6):349-355.
APA	Zhang, Peng,Zhai, Jiao,Gao, Xueyun,Zhao, Hongkang,Su, Wenyong,&Zhao, Lina.(2018).Targeted peptide-au cluster binds to epidermal growth factor receptor (egfr) in both active and inactive states: a clue for cancer inhibition through dual pathways.Science bulletin,63(6),349-355.
MLA	Zhang, Peng,et al."Targeted peptide-au cluster binds to epidermal growth factor receptor (egfr) in both active and inactive states: a clue for cancer inhibition through dual pathways".Science bulletin 63.6(2018):349-355.

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