药学学报, 2010, 45(1): 17-25
引用本文:
任锦 钦传光 徐春兰 王秋雨 左晓佳. 细胞穿膜肽作为药物载体的研究进展[J]. 药学学报, 2010, 45(1): 17-25.
LIN Jin, QIN Chuan-Guang, XU Chun-Lan, WANG Qiu-Yu, ZUO Xiao-Jia. Development of cell-penetrating peptides as vectors for drug delivery[J]. Acta Pharmaceutica Sinica, 2010, 45(1): 17-25.

细胞穿膜肽作为药物载体的研究进展
任 锦, 钦传光, 徐春兰, 王秋雨, 左晓佳
(西北工业大学生命科学院, 陕西 西安 710072)
摘要:

生物大分子在许多疾病的治疗中发挥着重要的作用, 但由于细胞膜的天然屏障作用, 只有分子质量小于600 Da的分子才能穿透细胞膜进入细胞内。这使得一些有治疗价值但无细胞膜穿透性的分子在细胞生物学、药学等领域的应用受到极大的限制。近年来发现的一些具有细胞穿透功能的短肽 (少于30个氨基酸) 即细胞穿膜肽 (CPPs), 能够有效地将蛋白质、多肽、核酸片段等以多种方式导入多种哺乳动物细胞, 其转导效率高且不会造成细胞损伤。CPPs的发现为生物大分子在细胞生物学、基因治疗、药物体内转运、临床药效评价以及细胞免疫学等研究领域等均具有良好的应用前景。本文就CPPs的种类特点、内化机制、应用及其存在的问题进行讨论和评述。

关键词:   
Development of cell-penetrating peptides as vectors for drug delivery
Abstract:

Biomacromolecules play an important role in the treatment of many diseases, but as a result of cell membrane serving as the natural barriers, only the small molecular compounds whose molecular weights are smaller than 600 Da can get through cell membrane and enter the cell.  In recent years, some short peptides (the length less than 30 amino acids) are found to have the cell-penetrating function, called cell-penetrating peptides (CPPs).  They are able to effectively translocate segments of protein, polypeptides, nucleic acid into the cells of many mammal animals with many methods.  They have high transduction efficiency and will not lead to cell damage.  So, the discovery of CPPs has a very good applicable prospect in such research fields as cell-biology, gene-therapy, drug transduction in vivo, evaluation of clinical medicine and medical immunology.  This    paper reviews the types and characteristics of CPPs, internalization mechanisms, applications, and their existing problems.

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