Abstract

Since the discovery of cell-penetrating peptides (CPP) in the 1980s, they have played a unique role in various fields owing to their excellent and unique cell membrane penetration function. In particular, in the treatment of tumours, CPPS have been used to deliver several types of ‘cargos’ to cancer cells. To address the insufficient targeting ability, non-selectivity, and blood instability, activatable cell-penetrating peptides, which can achieve targeted drug delivery in tumour treatment, enhance curative effects, and reduce toxicity have been developed. This study reviews the application of different cell-penetrating peptides in tumour-targeted delivery, overcoming multidrug resistance, organelle targeting, tumour imaging, and diagnosis, and summarises the different mechanisms of activatable cell-penetrating peptides in detail.

摘要

自1980年代发现细胞穿透肽(cell-penetrating peptides, CPP)以来，由于其优异而独特的细胞膜穿透功能，在各个领域发挥了独特的作用。特别是，在肿瘤治疗中，CPPS 已被用于向癌细胞输送多种类型的“货物”。针对靶向能力不足、非选择性和血液不稳定等问题，开发了可激活的细胞穿透肽，在肿瘤治疗中实现靶向给药、增强疗效、降低毒性。本研究回顾了不同细胞穿透肽在肿瘤靶向给药、克服多药耐药、细胞器靶向、肿瘤成像和诊断中的应用，并详细总结了可激活细胞穿透肽的不同机制。