Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors 
from the insect Blaps japanensis

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

doi:10.1016/j.bmcl.2012.04.027

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Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis

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Schneider, Bernd
Research Group Biosynthesis / NMR, MPI for Chemical Ecology, Max Planck Society;

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引用

Yan, Y.-M., Dai, H.-Q., Du, Y., Schneider, B., Guo, H., Li, D.-P., Zhang, L.-X., Fu, H., Dong, X.-P., & Cheng, Y.-X. (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. doi:10.1016/j.bmcl.2012.04.027.

引用: https://hdl.handle.net/11858/00-001M-0000-000F-A1FC-6

要旨

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 μM as determined by an ELISA assay, and 2.0 and 2.5 μM in an FP assay, respectively. These compounds represent the first example of natural small-molecule 14-3-3 inhibitors.