Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis
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; Cheng, Yong-Xian1,2
2012-06-15
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
卷号22期号:12页码:4179-4181
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.
关键词Blaps Japanensis Insects Phenolics 14-3-3 Protein-protein Interactions
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).
学科领域Pharmacology & Pharmacy ; Chemistry
DOI10.1016/j.bmcl.2012.04.027
收录类别SCI
语种英语
WOS研究方向Pharmacology & Pharmacy ; Chemistry
WOS类目Chemistry, Medicinal ; Chemistry, Organic
WOS记录号WOS:000304484600066
引用统计
被引频次:16[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/17605
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 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
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Yan, Yong-Ming,Dai, Huan-Qin,Du, Yuhong,et al. Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(12):4179-4181.
APA Yan, Yong-Ming.,Dai, Huan-Qin.,Du, Yuhong.,Schneider, Bernd.,Guo, Hui.,...&Cheng, Yong-Xian.(2012).Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(12),4179-4181.
MLA Yan, Yong-Ming,et al."Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 22.12(2012):4179-4181.
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