Replacement of a Proline with Silaproline Causes a 20-Fold Increase in the Cellular Uptake of a Pro-Rich Peptide
详细信息 查看全文
- 作者：Sí ; lvia Pujals ; Jimena Ferná ; ndez-Carneado ; Marcelo J. Kogan ; Jean Martinez ; Florine Cavelier ; and Ernest Giralt
- 刊名：Journal of the American Chemical Society
- 出版年：2006
- 出版时间：July 5, 2006
- 年：2006
- 卷：128
- 期：26
- 页码：8479 - 8483
- 全文大小：263K
- 年卷期：v.128,no.26(July 5, 2006)
- ISSN：1520-5126
文摘
The results presented here show that elementary design enhancements have led to a 20-foldincrease in the cellular uptake properties of a Pro-rich cell-penetrating peptide. These results are relevantnot only due to the increasing interest in using CPPs as molecular shuttles for intracellular drug deliverybut also because they illustrate the power of combining conformational analysis with rational design tomodulate the behavior of biologically active compounds.