Plasiatine, an Unprecedented Indole-Phenylpropanoid Hybrid from Plantago asiatica as a Potent Activator of the Nonreceptor Protein Tyrosine Phosphatase Shp2

doi:10.1038/srep24945

	Plasiatine, an Unprecedented Indole-Phenylpropanoid Hybrid from Plantago asiatica as a Potent Activator of the Nonreceptor Protein Tyrosine Phosphatase Shp2
	Gao, Zhong-Hua 1; Shi, Yi-Ming2 ; Qiang, Zhe 3; Wang, Xia 4; Shang, Shan-Zhai 1; Yang, Yan 1; Du, Bao-Wen 3; Peng, Hui-Pan 3; Ji, Xu1 ; Li, Honglin 4; Wang, Fei 3; Xiao, Wei-Lie 1
	2016-04-22
发表期刊	SCIENTIFIC REPORTS
卷号	6 期号:1 页码:24945
摘要	Plasiatine (1), isolated from the seeds of Plantago asiatica, is an unprecedented indole analogue linked to a phenylpropanoid moiety via a carbon bond that builds up a novel heteromeric construction with a C19N2 scaffold. Its structure was determined by spectroscopic data and computational evidence. Notably, experimental assay demonstrated that 1 significantly enhanced the activity of the nonreceptor protein tyrosine phosphatase Shp2 in vitro in a concentration-dependent manner with an EC50 value of 0.97 mu M, and activated phosphorylation of ERK, a known target of Shp2. Moreover, plasiatine (1) promoted hepatocellular HepG2 cells migration. Molecular docking suggested that plasiatine (1) binds to the catalytic cleft of Shp2. These results identified plasiatine (1) as the first small molecule Shp2 activator, and it warrants further investigation as a novel pharmaceutical tool to study the function of Shp2 in tumorigenesis.
DOI	10.1038/srep24945
收录类别	SCI
语种	英语
WOS记录号	WOS:000374752400001
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/26238
专题	植物化学与西部植物资源持续利用国家重点实验室
作者单位	1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China 2.Guangdong Prov Acad Chinese Med Sci, Guangzhou 510006, Guangdong, Peoples R China 3.Chinese Acad Sci, Chengdu Inst Biol, Chengdu 610041, Peoples R China 4.E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China
推荐引用方式 GB/T 7714	Gao, Zhong-Hua,Shi, Yi-Ming,Qiang, Zhe,et al. Plasiatine, an Unprecedented Indole-Phenylpropanoid Hybrid from Plantago asiatica as a Potent Activator of the Nonreceptor Protein Tyrosine Phosphatase Shp2[J]. SCIENTIFIC REPORTS,2016,6(1):24945.
APA	Gao, Zhong-Hua.,Shi, Yi-Ming.,Qiang, Zhe.,Wang, Xia.,Shang, Shan-Zhai.,...&Xiao, Wei-Lie.(2016).Plasiatine, an Unprecedented Indole-Phenylpropanoid Hybrid from Plantago asiatica as a Potent Activator of the Nonreceptor Protein Tyrosine Phosphatase Shp2.SCIENTIFIC REPORTS,6(1),24945.
MLA	Gao, Zhong-Hua,et al."Plasiatine, an Unprecedented Indole-Phenylpropanoid Hybrid from Plantago asiatica as a Potent Activator of the Nonreceptor Protein Tyrosine Phosphatase Shp2".SCIENTIFIC REPORTS 6.1(2016):24945.

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