细胞穿透环肽  

Cell-Permeable Cyclic Peptides

作　　者：梁妍钰 唐姗[2] 郑基深[1,2] 

机构地区：[1]中国科学院强磁场科学中心,合肥230031 [2]清华大学化学系,北京100084

出　　处：《化学进展》2014年第11期1793-1800,共8页Progress in Chemistry

摘　　要：细胞穿透环肽能够穿透细胞膜,特异性地靶向细胞内靶标,并具有较好的体内稳定性,因而具备很好的成药性,并受到研究者越来越多的关注。目前,主要有两种方式获得细胞穿透环肽,即从天然产物中获得和对已有的环肽或线性肽进行化学修饰。本文主要对上述两方面进行简要综述,重点介绍两类细胞穿透环肽天然产物以及通过化学修饰方法得到细胞穿透环肽的策略,并探讨细胞穿透环肽的结构-活性关系及其细胞穿透机理。Cyclic peptides are of considerable interest as potential protein ligands. Cell-permeable cyclic peptides receive much attention as peptide-based drugs ow ing to its cell permeability,specific targeting,and excellent stability in vivo. Nowadays,the researchers w orking on cell-permeable cyclic peptides focus on the issues as follow ： new cell-permeable cyclic peptides from natural products and their structure-activity relationships,and the chemical modifications of cyclic or linear peptides to artificially obtain cell-permeable cyclic peptides. Here,we review the issues mentioned above. This article is arranged in two sections. The first section introduces tw o kinds of discovered natural products as cell-permeable cyclic peptides; the second section covers the strategies of modifying cyclic or linear peptides into cell-permeable cyclic peptides and the insight of the structure-activity relationship of cell-permeable cyclic peptides.

关 键 词：多肽药物 环肽 细胞穿透 化学合成 

分 类 号：O629.72[理学—有机化学] TQ463[理学—化学]