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

Item

ITEM ACTIONSEXPORT

Add to Basket

Local TagsRelease HistoryDetailsSummary

Released

Journal Article

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

MPS-Authors

/persons/resource/persons4159

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

External Resource

No external resources are shared

Fulltext (restricted access)

There are currently no full texts shared for your IP range.

Fulltext (public)

There are no public fulltexts stored in PuRe

Supplementary Material (public)

There is no public supplementary material available

Citation

Yan, Y.-M., Dai, H.-Q., Du, Y., Schneider, B., Guo, H., Li, D.-P., et al. (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.

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

Abstract

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.