Dohmen Christian, Wagner Ernst
Department of Pharmacy, Pharmaceutical Biotechnology, Centre for Drug Research, Ludwig-Maximilians-Universität, Munich, Germany.
Methods Mol Biol. 2011;683:453-63. doi: 10.1007/978-1-60761-919-2_32.
Cell-penetrating peptides (CPPs) are a very interesting class of molecules to be introduced in gene and siRNA vectors. They can be used to overcome one of the biggest hurdles in gene and siRNA delivery in vitro and in vivo, the transfer across cell membranes. This chapter describes protocols for the synthesis and biological evaluation of a polylysine-based polymer. In this carrier system, melittin is used as CPP with a high activity to disrupt membranes. pH-Labile masking is applied to render the lytic activity specific for intracellular acidic endolysosomal organelles.
细胞穿透肽（CPPs）是一类非常有趣的分子，可被引入基因和小干扰RNA（siRNA）载体中。它们可用于克服体外和体内基因及siRNA递送过程中最大的障碍之一，即穿过细胞膜。本章描述了一种基于聚赖氨酸的聚合物的合成及生物学评估方案。在该载体系统中，蜂毒肽用作具有高膜破坏活性的细胞穿透肽。采用pH敏感屏蔽策略使裂解活性对细胞内酸性溶酶体细胞器具有特异性。
