Document Report Card
Basic Information
ID: ALA2029347
Journal: Bioorg Med Chem Lett
Title: Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis.
Authors: Yan YM, Dai HQ, Du Y, Schneider B, Guo H, Li DP, Zhang LX, Fu H, Dong XP, Cheng YX.
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 IC(50) 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.
CiteXplore: 22578460