He Fan, Cao Li, Zhang Xue-Jing, Xiang Bai, Cao De-Ying, Qi Xian-Rong
Yao Xue Xue Bao. 2015 Feb;50(2):141-7.
Cell-penetrating peptides (CPPs) offer a non-selective and receptor-independent mode to promote cellular uptake. Although the non-specificity of CPP-mediated internalization allows this approach applicable to a wide range of tumor types potentially, their universality is a significant obstacle to their clinical utility for targeted delivery of cancer therapeutics and imaging agents. Accordingly, many reports have focused on selective switching of systemically delivered inert CPPs into their active form in lesions (tumor). In this review, our attention is mainly confined to such an enzyme-sensitive domain incorporated delivery system with activatable CPPs (ACPPs), which have displayed the exciting strength in balancing the CPPs' pros and cons, and potential in the treatment and diagnosis of some diseases.
细胞穿透肽（CPPs）提供了一种非选择性且不依赖受体的方式来促进细胞摄取。尽管CPP介导的内化作用的非特异性使得这种方法有可能适用于多种肿瘤类型，但其普遍性是其在癌症治疗药物和成像剂靶向递送的临床应用中的一个重大障碍。因此，许多报告都集中在将全身递送的惰性CPPs在病变部位（肿瘤）选择性地转变为其活性形式。在这篇综述中，我们的注意力主要局限于这种带有可激活CPPs（ACPPs）的酶敏感域掺入递送系统，其在平衡CPPs的优缺点方面展现出令人兴奋的优势，并且在某些疾病的治疗和诊断中具有潜力。
