Membranotropic Cell Penetrating Peptides: The Outstanding Journey.
Membranotropic Cell Penetrating Peptides: The Outstanding Journey.
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膜促细胞穿透肽： 杰出之旅。
DOI：
10.3390/ijms161025323
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发表时间：
2015-10-23
影响因子：
5.6
通讯作者：
Galdiero S
中科院分区：
文献类型：
--
作者：
Falanga A;Galdiero M;Galdiero S
双层膜界定了单个细胞的内部，并为它们提供了生存和正常运作的能力。然而，细胞膜的穿越构成了进入细胞的主要障碍，并且许多药物的潜在治疗应用主要取决于递送工具的开发，该工具应选择性地将药物有效地输送至靶细胞，且毒性最小。细胞穿透肽很短，碱性肽因其在体外和体内跨膜递送货物的能力而被广泛使用。人们普遍认为其摄取机制主要涉及内吞途径，药物被捕获于内涵体和溶酶体内，只有少量能够到达细胞内靶点。在这种广泛的情况下，一个令人着迷的新假设是，亲膜肽可以有效地穿过生物膜，促进脂膜重组过程，并引起膜双层的局部和暂时的不稳定和重组，也可能能够进入细胞，绕过内体截留；特别是，通过促进内体逃逸或直接易位。本综述总结了用于药物输送的促膜肽的当前数据。
The membrane bilayer delimits the interior of individual cells and provides them with the ability to survive and function properly. However, the crossing of cellular membranes constitutes the principal impediment to gaining entry into cells, and the potential therapeutic application of many drugs is predominantly dependent on the development of delivery tools that should take the drug to target cells selectively and efficiently with only minimal toxicity. Cell-penetrating peptides are short and basic peptides are widely used due to their ability to deliver a cargo across the membrane both in vitro and in vivo. It is widely accepted that their uptake mechanism involves mainly the endocytic pathway, the drug is catched inside endosomes and lysosomes, and only a small quantity is able to reach the intracellular target. In this wide-ranging scenario, a fascinating novel hypothesis is that membranotropic peptides that efficiently cross biological membranes, promote lipid-membrane reorganizing processes and cause a local and temporary destabilization and reorganization of the membrane bilayer, may also be able to enter cells circumventing the endosomal entrapment; in particular, by either favoring the escape from the endosome or by direct translocation. This review summarizes current data on membranotropic peptides for drug delivery.