Cellular Translocation of a 纬-AApeptide Mimetic of Tat Peptide
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- 作者：Youhong Niu ; Ge Bai ; Haifan Wu ; Rongsheng E. Wang ; Qiao Qiao ; Shruti Padhee ; Robert Buzzeo ; Chuanhai Cao ; Jianfeng Cai
- 刊名：Molecular Pharmaceutics
- 出版年：2012
- 出版时间：May 7, 2012
- 年：2012
- 卷：9
- 期：5
- 页码：1529-1534
- 全文大小：339K
- 年卷期：v.9,no.5(May 7, 2012)
- ISSN：1543-8392
文摘
Cell-penetrating peptides including the trans-activating transcriptional activator (Tat) from HIV-1 have been used as carriers for intracellular delivery of a myriad of cargoes including drugs, molecular probes, DNAs and nanoparticles. Utilizing fluorescence flow cytometry and confocal fluorescence microscopy, we demonstrate that a 纬-AApeptide mimetic of Tat (48鈥?7) can cross the cell membranes and enter the cytoplasm and nucleus of cells, with efficiency comparable to or better than that of Tat peptide (48鈥?7). Deletion of the four side chains of the 纬-AApeptide attenuates translocation capability. We also establish that the 纬-AApeptide is even less toxic than the Tat peptide against mammalian cells. In addition to their low toxicity, 纬-AApeptides are resistant to protease degradation, which may prove to be advantageous over 伪-peptides for further development of molecular transporters for intracellular delivery.