Ma Minghai, Zhao Ruizhao, Li Xing, Jing Minxuan, Song Rundong, Fan Jinhai
Department of Urology, The First Affiliated Hospital, Xi'an Jiaotong University, Xi'an, 710061, China.
Clinical Medical School, Xi'an Medical University, Xi'an, 710061, China.
Curr Drug Deliv. 2025;22(4):387-400. doi: 10.2174/1567201820666230417083350.
Cell-penetrating peptides (CPPs) comprise short peptides of fewer than 30 amino acids, which are rich in arginine (Arg) or lysine (Lys). CPPs have attracted interest in the delivery of various cargos, such as drugs, nucleic acids, and other macromolecules over the last 30 years. Among all types of CPPs, arginine-rich CPPs exhibit higher transmembrane efficiency due to bidentate bonding between their guanidinium groups and negatively charged cellular components. Besides, endosome escape can be induced by arginine-rich CPPs to protect cargo from lysosome-dependent degradation. Here we summarize the function, design principles, and penetrating mechanisms of arginine-rich CPPs, and outline their biomedical applications in drug delivery and biosensing in tumors.
细胞穿透肽（CPPs）由少于30个氨基酸的短肽组成，这些短肽富含精氨酸（Arg）或赖氨酸（Lys）。在过去30年里，CPPs在递送各种货物（如药物、核酸和其他大分子）方面引起了人们的兴趣。在所有类型的CPPs中，富含精氨酸的CPPs由于其胍基与带负电荷的细胞成分之间的双齿键合而表现出更高的跨膜效率。此外，富含精氨酸的CPPs可以诱导内体逃逸，以保护货物免受溶酶体依赖性降解。在这里，我们总结了富含精氨酸的CPPs的功能、设计原则和穿透机制，并概述了它们在肿瘤药物递送和生物传感中的生物医学应用。
