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

  • Bioorg Med Chem Lett. 2012 Jun 15;22(12):4179-81. doi: 10.1016/j.bmcl.2012.04.027.
Yong-Ming Yan  1 ,  Huan-Qin Dai ,  Yuhong Du ,  Bernd Schneider ,  Hui Guo ,  Dian-Peng Li ,  Li-Xin Zhang ,  Haian Fu ,  Xiao-Ping Dong ,  Yong-Xian Cheng
Affiliations
  • 1. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, PR China.
PMID: 22578460 DOI: 10.1016/j.bmcl.2012.04.027
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.

Products