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How to overcome endosomal entrapment of cell‐penetrating peptides to release the therapeutic potential of peptides?
Peptide Science ( IF 1.5 ) Pub Date : 2020-05-07 , DOI: 10.1002/pep2.24168 Ferran Nadal‐Bufí 1 , Sónia Troeira Henriques 1
Peptide Science ( IF 1.5 ) Pub Date : 2020-05-07 , DOI: 10.1002/pep2.24168 Ferran Nadal‐Bufí 1 , Sónia Troeira Henriques 1
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Peptides gained a renascent interest as alternative pharmaceuticals, and in particular as anticancer drugs to inhibit intracellular proteins involved in cancer pathways, inaccessible to other pharmaceutical agents. However, the use of peptides as therapeutics is still limited by difficulties in reaching the protein target located in the cytosol. Cell penetrating peptides (CPPs) are being explored as tools to deliver therapeutic peptides inside cells, but they often enter cells using endocytic pathways and become entrapped inside endosomes. Therefore, a strategy to unleash the potential of peptides as therapeutics is to control the release of CPPs from endosomes. In this review we summarize recent strategies employed to improve endosomal escape of CPPs. Lessons learned from these studies can guide the design of CPPs as tools to deliver peptide sequences able to inhibit cancer targets and accelerate their development as therapeutics.
中文翻译：
如何克服细胞穿透肽的内体包裹，释放肽的治疗潜力？
肽作为替代药物，特别是作为抑制癌症途径中涉及的细胞内蛋白质的抗癌药物，引起了人们的广泛兴趣，而其他药物则无法使用。然而，由于难以达到位于胞质溶胶中的蛋白质靶标，因此肽作为治疗剂的用途仍然受到限制。细胞穿透肽（CPPs）正在探索作为在细胞内传递治疗性肽的工具，但它们通常通过内吞途径进入细胞并被内体包裹。因此，释放肽作为治疗剂的潜力的策略是控制CPP从内体释放。在这篇综述中，我们总结了用于改善CPP内体逸出的最新策略。
更新日期：2020-05-07
中文翻译：
如何克服细胞穿透肽的内体包裹，释放肽的治疗潜力？
肽作为替代药物，特别是作为抑制癌症途径中涉及的细胞内蛋白质的抗癌药物，引起了人们的广泛兴趣，而其他药物则无法使用。然而，由于难以达到位于胞质溶胶中的蛋白质靶标，因此肽作为治疗剂的用途仍然受到限制。细胞穿透肽（CPPs）正在探索作为在细胞内传递治疗性肽的工具，但它们通常通过内吞途径进入细胞并被内体包裹。因此，释放肽作为治疗剂的潜力的策略是控制CPP从内体释放。在这篇综述中，我们总结了用于改善CPP内体逸出的最新策略。
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