| 论文题目: | Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis |
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| 作者: | Yan, YM; Dai, HQ; Du, YH; Schneider, B; Guo, H; Li, DP; Zhang, LX; Fu, HA; Dong, XP; Cheng, YX |
| 联系作者: | Cheng, YX |
| 刊物名称: | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS |
| 期: | 12 |
| 卷: | 22 |
| 页: | 4179-4181 |
| 年份: | 2012 |
| 影响因子: | 2.554 |
| 论文下载: | 下载地址 |
| 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. |
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