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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
Citation statistics:
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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