多肽介导的生物活性分子细胞靶向及胞内运输策略  

Strategies for cellular targeting of biomacromolecules and intracellular delivery mediated by polypeptides

作　　者：王琥[1] 柳长柏[1] 

机构地区：[1]三峡大学分子生物学研究所,湖北宜昌443002

出　　处：《中国新药与临床杂志》2009年第7期486-490,共5页Chinese Journal of New Drugs and Clinical Remedies

基　　金：国家自然科学基金项目(20774094/B040203)

摘　　要：细胞膜屏障在保护细胞正常形态和功能的同时,也使很多有治疗作用的生物活性分子难以进入细胞内,使其应用受到极大限制。目前常用的向细胞内导入生物大分子的方式主要有电穿孔和脂质体转染等,但因其对细胞有较大毒性而多局限于体外实验研究。近年来,基于多肽的药物输送载体以其安全性、低毒性、低免疫反应性、靶向性及易于组装等优点被寄予厚望。本文就多肽在生物活性分子胞内运输过程、提高输送效率的策略作一综述。Recent advances in the understanding of cellular and molecular mechanisms were underlying the development of new potential molecular therapy targets, and together with the advances in bioteehnology, increased the appeal and importance of various biomacromoleeules such as DNA, RNA, peptides, proteins and their mimics as therapeutic agents. In order to exert their biological action, biomaeromolecules had to be delivered into specific intracellular compartments usually. The requirement for cytoplasmic or nuclear delivery posed a major challenge for the development of effective intracellular therapies based on the use of high molecular weight drugs because of the hydrophobie nature of the plasma membrane surrounding the cell, which effectively restricted the free exchange of hydrophilic molecules between the cellular interior and the extraeellular medium. There were a growing number of reports showing the usefulness of polypeptides for intraeellular delivery of macromoleenles. As the backbone of drug vectors, polypeptides played an important role in target delivery, endosome escape, and nuclear transport and so on. Applications of polypeptides delivery systems used in different areas such as vaccine development, cancer immunotherapy, gene delivery, and cellular imaging.

关 键 词：肽类 溶酶体 配体 核定位信号 细胞穿透肽 药物输送 

分 类 号：R966[医药卫生—药理学]