Total synthesis of snake toxin α-bungarotoxin and its analogues by hydrazide-based native chemical ligation  

作　　者：Xiao-Qi Guo Jun Liang Ying Li Yong Zhang Dongliang Huang Changlin Tian 

机构地区：[1]High Magnetic Field Laboratory, Chinese Academy of Sciences [2]School of Life Science,University of Science and Technology of China [3]Department of Chemistry,University of Science and Technology of China

出　　处：《Chinese Chemical Letters》2018年第7期1139-1142,共4页中国化学快报（英文版）

基　　金：supported by the Science and Technological Fund of Anhui Province for Outstanding Youth(No. 1808085J04);the Innovative Program Development Foundation Hefei Center Physical Science Technology(No. 2017FXCX002)

摘　　要：Nicotinic acetylcholine receptors(nAChRs) play important roles in intercellular communications of nerve cells. α-Bungarotoxins(αBtx) is a moderator for the nAChRs. Chemical synthesis provides a promising way to access aBtx and their analogues. Here, we reported a new method for a-bungarotoxin by combining Fmoc-SPPS and peptide hydrazide based ligation strategy. The two-segment ligation method may enable efficient synthesis of aBtx analogues. These synthetic toxin peptides are useful tools for development of imaging or therapeutic reagents.Nicotinic acetylcholine receptors(nAChRs) play important roles in intercellular communications of nerve cells. α-Bungarotoxins(αBtx) is a moderator for the nAChRs. Chemical synthesis provides a promising way to access aBtx and their analogues. Here, we reported a new method for a-bungarotoxin by combining Fmoc-SPPS and peptide hydrazide based ligation strategy. The two-segment ligation method may enable efficient synthesis of aBtx analogues. These synthetic toxin peptides are useful tools for development of imaging or therapeutic reagents.

关 键 词：Chemical synthesis Native chemical ligation Peptide hydrazide Α-BUNGAROTOXIN Nicotinic acetylcholine receptors 

分 类 号：TQ460.1[化学工程—制药化工]