Functional peptides for siRNA delivery.
Functional peptides for siRNA delivery.
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DOI：
10.1016/j.addr.2016.08.004
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发表时间：
2017-02
影响因子：
16.1
通讯作者：
Gao X
中科院分区：
文献类型：
--
作者：
Tai W;Gao X
SiRNA被认为是一种有效的治疗剂，因为它在抑制疾病发展过程中过度表达的基因方面具有高度的特异性和效率。近二十年来，人们一直致力于将siRNA技术应用于临床。然而，到目前为止，仅取得了有限的成功，这主要是由于缺乏针对细胞类型的、安全和有效的递送技术来将siRNA携带到发生RNA干扰的靶细胞的胞浆中。在新兴的siRNA递送候选纳米载体中，多肽因其结构和功能的多样性而广受欢迎。已发现多种多肽能够通过不同的机制将siRNA转移到活细胞中，如直接穿透细胞膜、内吞作用介导的细胞进入随后的内吞作用和受体介导的摄取。本文综述了多肽在siRNA传递中所起的多种作用，如膜穿透、内小体破坏、靶向以及这些功能的结合。
siRNA is considered as a potent therapeutic agent because of its high specificity and efficiency in suppressing genes that are overexpressed during disease development. For nearly two decades, a significant amount of efforts has been dedicated to bringing the siRNA technology into clinical uses. However, only limited success has been achieved to date, largely due to the lack of a cell type-specific, safe, and efficient delivery technology to carry siRNA into the target cells' cytosol where RNA interference takes place. Among the emerging candidate nanocarriers for siRNA delivery, peptides have gained popularity because of their structural and functional diversity. A variety of peptides have been discovered for their ability to translocate siRNA into living cells via different mechanisms such as direct penetration through the cellular membrane, endocytosis-mediated cell entry followed by endosomolysis, and receptor-mediated uptake. This review is focused on the multiple roles played by peptides in siRNA delivery, such as membrane penetration, endosome disruption, targeting, as well as the combination of these functionalities.