细胞穿透肽在肿瘤治疗中的应用

随着人类对基因组信息解读的不断深入,越来越多的生物大分子作为候选药物进入生物治疗领域。但细胞表面的脂质双层膜具有选择通透性,这种天然屏障作用在保护细胞的同时也限制了绝大多数生物大分子进入细胞内部发挥治疗效应。目前流行的入胞转运方式如电穿孔、脂质体转染等均存在对细胞的额外毒副作用,且作用范围局限于体外实验。细胞穿透肽是一类以非受体依赖方式,非经典内吞方式直接穿过细胞膜进入细胞的多肽。它们可以与多种生物活性物质连接并携带其进入细胞,这一特性为它们成为理想的药物载体提供了可能。本文对使用细胞穿透肽作为载体转运具有抗癌作用的生物大分子进入细胞的抗癌实验予以介绍。

Cell penetrating peptides in cancer therapy

The genomic information obtained through the human genome project has been accelerating the analysis of the functions of various disease relevant genes. The high molecular weight biomolecules becomes increasingly important for the development of molecular therapies. However, the usage of such therapeutic macromolecules has been limited by the poor permeability across the lipid bilayer of the cellular plasma membrane. In order to overcome this barrier, several chemical and physical methods have been developed, such as electroporation and cationic lipids/liposomes. The drawbacks of these methods are the unwanted cellular effects and their limitation to in vitro applications. Cell penetrating peptides (CPPs) is a group of oligopeptides that could penetrate the cell membrane via a receptor-independent and non-endocytotic process with various conjungated bioactive molecules. Such ability makes them outstanding transmembrane vectors for various therapuetic biomolecules. In this review, we will introduce several representative strategies to develop antitumor macromolecules using CPPs.