Zorko Matjaz, Langel Ulo
Institute of Biochemistry, Medical Faculty, University of Ljubljana, Vrazov trg 2, SLO-1000, Ljubljana, Slovenia.
Adv Drug Deliv Rev. 2005 Feb 28;57(4):529-45. doi: 10.1016/j.addr.2004.10.010. Epub 2005 Jan 22.
Cell-penetrating peptides (CPPs) are short peptides of less than 30 amino acids that are able to penetrate cell membranes and translocate different cargoes into cells. The only common feature of these peptides appears to be that they are amphipathic and net positively charged. The mechanism of cell translocation is not known but it is apparently receptor and energy independent although, in certain cases, translocation can be partially mediated by endocytosis. Cargoes that are successfully internalized by CPPs range from small molecules to proteins and supramolecular particles. Most CPPs are inert or have very limited side effects. Their penetration into cells is rapid and initially first-order, with half-times from 5 to 20 min. The size of smaller cargoes does not affect the rate of internalization, but with larger cargoes, the rate is substantially decreased. CPPs are novel vehicles for the translocation of cargo into cells, whose properties make them potential drug delivery agents, of interest for future use.
细胞穿透肽（CPPs）是由少于30个氨基酸组成的短肽，能够穿透细胞膜并将不同的货物转运到细胞内。这些肽唯一的共同特征似乎是它们具有两亲性且带正电荷。细胞转运的机制尚不清楚，但显然与受体和能量无关，尽管在某些情况下，转运可部分由内吞作用介导。被CPPs成功内化的货物范围从小分子到蛋白质和超分子颗粒。大多数CPPs是惰性的或副作用非常有限。它们快速进入细胞，最初呈一级动力学，半衰期为5至20分钟。较小货物的大小不影响内化速率，但对于较大的货物，内化速率会大幅降低。CPPs是将货物转运到细胞内的新型载体，其特性使其成为潜在的药物递送剂，具有未来应用的价值。
