Solid-phase synthesis of neuroactive spider–wasp hybrid toxin analogues using a backbone amide linker
作者:Christian A. Olsen、Matthias Witt、Henrik Franzyk、Jerzy W. Jaroszewski
DOI:10.1016/j.tetlet.2006.11.074
日期:2007.1
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
从蜘蛛和黄蜂的毒液中分离的多胺毒素及其合成类似物是中枢神经系统和外周神经系统中非竞争性配体门控离子受体的拮抗剂,并已被证明可作为研究受体结构和功能的有价值的工具。在本信中,我们描述了使用BAL树脂的新型杂化毒素的有效固相合成(SPS)。该策略可实现毒素分子的双向构建,并且在化学类似的毒素类似物文库的SPS中具有用于结构-活性关系(SAR)研究的潜力。