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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Yan YM,Dai HQ,Du Y,Schneider B,Guo H,Li DP,Zhang LX,Fu H,Dong XP,Cheng YX

doi

10.1016/j.bmcl.2012.04.027

subject

Has Abstract

pub_date

2012-06-15 00:00:00

pages

4179-81

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00466-0

journal_volume

22

pub_type

杂志文章

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