Cell-penetrating peptides (CPPs) are short peptides that can penetrate the cell membrane or tissue barrier. CPPs can deliver a variety of biomacromolecules, such as proteins, RNA and DNA, into cells to produce intracellular functional effects. Endocytosis and direct penetration have been suggested as the two major uptake mechanisms for CPPs-mediated cargo delivery. Compared with other non-natural chemical molecules-based delivery reagents, the CPPs have better biocompatibility, lower cytotoxicity, are easily degraded after cargo delivery, and can be fused and recombined expressed with bioactive proteins. Because of these advantages, the CPPs have become an important potential tool for delivery of developing drugs which targets intracellular factors. As a novel delivery tool, the CPPs also show promising application prospects in biomedical researches. This review summarized recent advances regarding the classification characteristics, the cellular uptake mechanisms and therapeutic application potentials of CPPs.
细胞穿膜肽 (Cell-penetrating peptides，CPPs) 是一类能够穿过细胞膜或组织屏障的短肽。CPPs 可通过内吞和直接穿透等机制运载蛋白质、RNA、DNA 等生物大分子进入细胞内发挥其效应功能。相比于其他非天然的化学分子，CPPs 具有生物相容性佳、对细胞造成的毒性小、完成入胞转运后可降解、并能与生物活性蛋白直接融合重组表达等优点，因此成为以胞内分子为靶标的药物递送技术发展的重要工具，并在生物医学研究领域具有良好的应用前景。文中针对CPPs 的分类特点、入胞转运机制及其治疗应用的新近研究进展进行综述和讨论。.
Keywords: cell-penetrating delivery system; cell-penetrating peptides; cellular uptake mechanisms.