Plasiatine, an Unprecedented Indole-Phenylpropanoid Hybrid from Plantago asiatica as a Potent Activator of the Nonreceptor Protein Tyrosine Phosphatase Shp2
Gao, Zhong-Hua1; Shi, Yi-Ming2; Qiang, Zhe3; Wang, Xia4; Shang, Shan-Zhai1; Yang, Yan1; Du, Bao-Wen3; Peng, Hui-Pan3; Ji, Xu1; Li, Honglin4; Wang, Fei3; Xiao, Wei-Lie1
2016-04-22
Source PublicationSCIENTIFIC REPORTS
Volume6Issue:1Pages:24945
AbstractPlasiatine (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.
DOI10.1038/srep24945
Indexed BySCI
Language英语
WOS IDWOS:000374752400001
Citation statistics
Cited Times:6[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/26238
Collection植物化学与西部植物资源持续利用国家重点实验室
Affiliation1.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
Recommended Citation
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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