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
	Xiao, WL (reprint author), Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China.; Gao, ZH; Shi, YM; Qiang, Z; Wang, X; Shang, SZ; Yang, Y; Du, BW; Wang, F (reprint author), Chinese Acad Sci, Chengdu Inst Biol, Chengdu 610041, Peoples R China.; Li, HL (reprint author), E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China.
刊名	SCIENTIFIC REPORTS
	2016
卷号	6 页码:24945（1-9）
DOI	10.1038/srep24945
产权排序	3
文献子类	Article
英文摘要	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.
学科主题	Science & Technology - Other Topics
资助项目	Shi, Yi-Ming/0000-0001-6933-4971
项目编号	Shi, Yi-Ming/K-1204-2014 ; Li, Honglin/F-2606-2010
语种	英语
资助机构	NSFC [81422046] ; NSFC [81422046] ; NSF of Yunnan Province [2012FB178] ; NSF of Yunnan Province [2012FB178] ; SRF for ROCS, SEM ; SRF for ROCS, SEM ; HPC Center of KIB, CAS ; HPC Center of KIB, CAS ; NSFC [81422046] ; NSFC [81422046] ; NSF of Yunnan Province [2012FB178] ; NSF of Yunnan Province [2012FB178] ; SRF for ROCS, SEM ; SRF for ROCS, SEM ; HPC Center of KIB, CAS ; HPC Center of KIB, CAS
内容类型	期刊论文
源URL	[http://210.75.237.14/handle/351003/28198]
专题	成都生物研究所_天然产物研究
通讯作者	Xiao, WL (reprint author), Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China.; Wang, F (reprint author), Chinese Acad Sci, Chengdu Inst Biol, Chengdu 610041, Peoples R China.; Li, HL (reprint author), 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	Xiao, WL ,Gao, ZH,Shi, YM,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,2016,6:24945（1-9）.
APA	Xiao, WL .,Gao, ZH.,Shi, YM.,Qiang, Z.,Wang, X.,...&Xiao, WL.(2016).Plasiatine, an Unprecedented Indole-Phenylpropanoid Hybrid from Plantago asiatica as a Potent Activator of the Nonreceptor Protein Tyrosine Phosphatase Shp2.SCIENTIFIC REPORTS,6,24945（1-9）.
MLA	Xiao, WL ,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(2016):24945（1-9）.