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

doi:10.1016/j.scib.2018.02.007

	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, P; Zhao, HK; Gao, XY; Zhai, J; 张鹏(多2); Zhai J(翟皎); Zhao LN(赵丽娜); Su, WY; Zhao, LN
刊名	SCIENCE BULLETIN
	2018
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
文献子类	Article
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.
电子版国际标准刊号	2095-9281
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
语种	英语
CSCD记录号	CSCD:6217629
WOS记录号	WOS:000429784000006
内容类型	期刊论文
源URL	[http://ir.ihep.ac.cn/handle/311005/285809]
专题	高能物理研究所_多学科研究中心
通讯作者	Zhao LN(赵丽娜)
作者单位	中国科学院高能物理研究所
推荐引用方式 GB/T 7714	Zhang, P,Zhao, HK,Gao, XY,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, P.,Zhao, HK.,Gao, XY.,Zhai, J.,张鹏.,...&Zhao, LN.(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, P,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.