Different stapling-based peptide drug design:Mimicking α-helix as inhibitors of protein-protein interaction  

作　　者：Xiang Li Yan Zou Hong-Gang Hu 

机构地区：[1]School of Pharmacy, Second Military Medical University

出　　处：《Chinese Chemical Letters》2018年第7期1088-1092,共5页中国化学快报（英文版）

摘　　要：Peptide stapling strategy has been proven a promising solution in addressing two major pharmacological hurdles, proteolytic stability and membrane permeability, for small peptides as therapeutics. This stapling peptides feature a covalent cross-link of side chains, thus effectively mimicking α-helix as inhibitors of protein-protein interactions. In this review, we category and analyze key examples of various peptide stapling strategies based on different cross-links aligned on the side chain of peptides mainly in the last three years.Peptide stapling strategy has been proven a promising solution in addressing two major pharmacological hurdles, proteolytic stability and membrane permeability, for small peptides as therapeutics. This stapling peptides feature a covalent cross-link of side chains, thus effectively mimicking α-helix as inhibitors of protein-protein interactions. In this review, we category and analyze key examples of various peptide stapling strategies based on different cross-links aligned on the side chain of peptides mainly in the last three years.

关 键 词：STAPLING PEPTIDE Α-HELIX Protein-protein interaction 

分 类 号：TQ464.7[化学工程—制药化工]