Extensive research has been undertaken in the pursuit of anticancer therapeutics. Many anticancer drugs require specificity of delivery to cancer cells, whilst sparing healthy tissue. Cell-penetrating peptides (CPPs), now well established as facilitators of intracellular delivery, have in recent years advanced to incorporate target specificity and thus possess great potential for the targeted delivery of anticancer cargoes. Though none have yet been approved for clinical use, this novel technology has already entered clinical trials. In this review we present CPPs, discuss their classification, mechanisms of cargo internalization and highlight strategies for conjugation to anticancer moieties including their incorporation into therapeutic proteins. As the mainstay of this review, strategies to build specificity into tumor targeting CPP constructs through exploitation of the tumor microenvironment and the use of tumor homing peptides are discussed, whilst acknowledging the extensive contribution made by CPP constructs to target specific protein–protein interactions integral to intracellular signaling pathways associated with tumor cell survival and progression. Finally, antibody/antigen CPP conjugates and their potential roles in cancer immunotherapy and diagnostics are considered. In summary, this review aims to harness the potential of CPP-aided drug delivery for future cancer therapies and diagnostics whilst highlighting some of the most recent achievements in selective delivery of anticancer drugs, including cytostatic drugs, to a range of tumor cells both in vitro and in vivo.

在追求抗癌治疗方面进行了广泛的研究。许多抗癌药物需要特异性递送至癌细胞，同时保留健康组织。细胞穿透肽 (CPPs)，现在已被确立为细胞内递送的促进剂，近年来已经发展到结合靶特异性，因此具有靶向递送抗癌货物的巨大潜力。尽管尚未批准临床使用，但这项新技术已经进入临床试验阶段。在这篇综述中，我们介绍了 CPP，讨论了它们的分类、货物内化机制，并强调了与抗癌部分结合的策略，包括它们与治疗性蛋白质的结合。作为本次评测的主要内容，讨论了通过利用肿瘤微环境和使用肿瘤归巢肽在肿瘤靶向 CPP 构建体中建立特异性的策略，同时承认 CPP 构建体对靶向与肿瘤细胞相关的细胞内信号通路不可或缺的特定蛋白质-蛋白质相互作用的广泛贡献生存和进展。最后，考虑了抗体/抗原 CPP 偶联物及其在癌症免疫治疗和诊断中的潜在作用。总之，这篇综述旨在利用 CPP 辅助药物递送在未来癌症治疗和诊断中的潜力，同时强调一些最近在选择性递送抗癌药物（包括细胞抑制药物）到一系列肿瘤细胞方面的成就 同时承认 CPP 构建体对靶向与肿瘤细胞存活和进展相关的细胞内信号通路不可或缺的特定蛋白质-蛋白质相互作用做出的广泛贡献。最后，考虑了抗体/抗原 CPP 偶联物及其在癌症免疫治疗和诊断中的潜在作用。总之，这篇综述旨在利用 CPP 辅助药物递送在未来癌症治疗和诊断中的潜力，同时强调一些最近在选择性递送抗癌药物（包括细胞抑制药物）到一系列肿瘤细胞方面的成就 同时承认 CPP 构建体对靶向与肿瘤细胞存活和进展相关的细胞内信号通路不可或缺的特定蛋白质-蛋白质相互作用做出的广泛贡献。最后，考虑了抗体/抗原 CPP 偶联物及其在癌症免疫治疗和诊断中的潜在作用。总之，这篇综述旨在利用 CPP 辅助药物递送在未来癌症治疗和诊断中的潜力，同时强调一些最近在选择性递送抗癌药物（包括细胞抑制药物）到一系列肿瘤细胞方面的成就 考虑了抗体/抗原 CPP 偶联物及其在癌症免疫治疗和诊断中的潜在作用。总之，这篇综述旨在利用 CPP 辅助药物递送在未来癌症治疗和诊断中的潜力，同时强调一些最近在选择性递送抗癌药物（包括细胞抑制药物）到一系列肿瘤细胞方面的成就 考虑了抗体/抗原 CPP 偶联物及其在癌症免疫治疗和诊断中的潜在作用。总之，这篇综述旨在利用 CPP 辅助药物递送在未来癌症治疗和诊断中的潜力，同时强调一些最近在选择性递送抗癌药物（包括细胞抑制药物）到一系列肿瘤细胞方面的成就体外和体内。