| 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 | |
| 通讯作者 | Cheng, YX (reprint author), Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China,lzhang03@gmail.com ; hfu@emory.edu ; yxcheng@mail.kib.ac.cn |
| 2012-06-15 | |
| 发表期刊 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| ISSN | 0960-894X |
| 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 |
| 学科领域 | Pharmacology & Pharmacy ; Chemistry |
| DOI | 10.1016/j.bmcl.2012.04.027 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000304484600066 |
| 引用统计 | |
| 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 |
| 推荐引用方式 GB/T 7714 | 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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