Solid-phase synthesis of neuroactive spider-wasp hybrid toxin analogues using a backbone amide linker

摘要

Polyamine toxins isolated from the venoms of spiders and wasps and their synthetic analogues are uncompetitive antagonists of ligand-gated ionotropic receptors in the central-and peripheral nervous systems,and have proved valuable as tools for the investigation of receptor structure and function.In the present letter we describe the efficient solid-phase synthesis(SPS)of novel hybrid toxins using a BAL resin.This strategy enables the bidirectional construction of toxin molecules and has a potential in SPS of chemically diverse libraries of toxin analogues for structure-activity relationship(SAR)studies.