Cell-penetrating cis-γ-amino-L-proline-derived peptides
Cell-penetrating cis-γ-amino-L-proline-derived peptides
复制标题
DOI：
10.1021/ja051648k
复制
发表时间：
2005-07-06
影响因子：
15
通讯作者：
Royo, M
中科院分区：
文献类型：
--
作者：
Farrera-Sinfreu, J;Giralt, E;Royo, M
本文描述了在脯氨酸a胺上功能化的顺- γ -氨基- l -脯氨酸低聚物的合成，这些低聚物具有模拟天然氨基酸侧链的几个基团，包括丙氨酸、亮氨酸和苯丙氨酸。这些γ肽通过内吞机制进入不同的细胞系（COS-1和HeLa）。通过平板荧光法、流式细胞术和共聚焦显微镜研究了这些化合物在37℃和4℃下被细胞吸收的能力。除了它们的细胞摄取能力外，这些非天然的短长度低聚物比众所周知的穿透性TAT肽具有优势，例如比TAT毒性更小和蛋白酶抗性。
The synthesis of cis-gamma-amino-L-proline oligomers functionalized at the proline a-amine with several groups that mimic the side chains of natural amino acids, including alanine, leucine, and phenylalanine, is herein described. These gamma-peptides enter into different cell lines (COS-1 and HeLa) via an endocytic mechanism. The ability of these compounds to be taken up into cells was studied at 37 degrees C and 4 degrees C by plate fluorimetry, flow cytometry, and confocal microscopy. In addition to their capacity for cellular uptake, these unnatural short length oligomers offer advantages over the well-known penetrating TAT peptide, such as being less toxic than TAT and protease resistance.