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题名: Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis
作者: Yan, Yong-Ming1, 2; Dai, Huan-Qin3; Du, Yuhong4, 5; Schneider, Bernd6; Guo, Hui3; Li, Dian-Peng7; Zhang, Li-Xin1, 3; Fu, Haian1, 4, 5; Dong, Xiao-Ping2; null(程永现)1, 2
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
关键词: Blaps japanensis ; Insects ; Phenolics ; 14-3-3 Protein-protein interactions
英文摘要: In this study, we report three novel naturally occurring compounds, blapsins A (1) and B (2), and blapsamide (3) from the ethanol extract of the stink beetle, Blaps japanensis. The structures of these compounds were determined using spectroscopic methods. Compound 3 is a phenolic compound bearing a formamido group in the structure. Functional studies revealed that compounds 1 and 2 potently inhibited 14-3-3 protein-protein interactions (PPIs) with IC50 values of 9.2 and 10.0 mu M as determined by an ELISA assay, and 2.0 and 2.5 mu M in an FP assay, respectively. These compounds represent the first example of natural small-molecule 14-3-3 inhibitors. (C) 2012 Elsevier Ltd. All rights reserved.
出版日期: 2012-06-15
卷号: 22, 期号:12, 页码:4179-4181
DOI标识: 10.1016/j.bmcl.2012.04.027
语种: 英语
ISSN号: 0960-894X
资助信息: This work was financially supported by the following Grants: National Natural Science Foundation of China (No. 21172223), Sino-German International Collaboration Project from Yunnan Province (No. 2009AC011), the Open Research Fund of the State Key Laboratory Breeding Base of Systematic Research, Development and Utilization of Chinese Medicine Resources, and Project of Natural Compound Library Construction from Chinese Academy of Sciences (KSCX2-EW-R-15).
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内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/17605
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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作者单位: 1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China
2.Chengdu Univ Tradit Chinese Med, Coll Pharm, Chengdu 610075, Peoples R China
3.Chinese Acad Sci, Inst Microbiol, Beijing 100101, Peoples R China
4.Emory Univ, Sch Med, Dept Pharmacol, Atlanta, GA 30322 USA
5.Emory Univ, Sch Med, Emory Chem Biol Discovery Ctr, Atlanta, GA 30322 USA
6.Max Planck Inst Chem Ecol, D-07745 Jena, Germany
7.Guangxi Inst Bot, Guangxi Key Lab Funct Phytochem Res & Utilizat, Guilin 541006, Peoples R China

Recommended Citation:
Yan,Yong-Ming;Dai,Huan-Qin;Du,Yuhong;Schneider,Bernd;Guo,Hui;Li,Dian-Peng;Zhang,Li-Xin;Fu,Haian;Dong,Xiao-Ping;Cheng,Yong-Xian.Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis,BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(12):4179-4181
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