Institute for Chemical Research, Kyoto University, Uji, Kyoto 611-0011, Japan.
J Control Release. 2009 Sep 1;138(2):128-33. doi: 10.1016/j.jconrel.2009.05.019. Epub 2009 May 22.
Cell penetrating peptides (CPPs), including arginine-rich peptides, are attractive tools for the intracellular delivery of various bioactive molecules with a low membrane permeability. We showed that the accelerated intracellular delivery of arginine-rich peptides was achieved by the addition of a short peptide segment (penetration accelerating sequence, Pas) to arginine-rich CPPs. The cytosolic release of the Pas-attached arginine-rich CPPs was observed within 5 min after the treatment of the cells with the peptides even in the presence of serum. Effectiveness of the Pas segment in the intracellular delivery of bioactive peptides using arginine-rich CPPs was exemplified through the enhanced growth inhibition activity of the malignant glioma cells by a retro-inverso peptide derived from the p53 C-terminal 22-amino-acid segment (positions 361-382).
细胞穿透肽（CPPs），包括富含精氨酸的肽，是一种有吸引力的工具，可将各种具有低膜通透性的生物活性分子递送到细胞内。我们表明，通过向富含精氨酸的 CPP 添加短肽段（穿透加速序列，Pas），可以实现富含精氨酸的肽的加速细胞内递送。在用肽处理细胞后 5 分钟内，甚至在存在血清的情况下，也可以观察到与 Pas 连接的富含精氨酸的 CPP 的细胞质释放。通过增强源自 p53 C 末端 22 个氨基酸片段（位置 361-382）的 retro-inverso 肽对恶性神经胶质瘤细胞的生长抑制活性，证明了 Pas 片段在使用富含精氨酸的 CPP 进行生物活性肽的细胞内递送中的有效性。
