Peptoidic Amino- and Guanidinium-Carrier Systems: Targeted Drug Delivery into the Cell Cytosol or the Nucleus
作者:Tina Schröder、Nicole Niemeier、Sergii Afonin、Anne S. Ulrich、Harald F. Krug、Stefan Bräse
DOI:10.1021/jm070603m
日期:2008.2.1
Efficient drug delivery is essential for many therapeutic applications. Some cell-penetrating peptides, peptide mimetics, and peptoids express transport function that, however, lack in most cases specific intracellular destination. In this study, carrier-peptoids with either amino or guanidinium side chains, were investigated with regard to their cellular uptake, toxicity, and intracellular localization. Transport specifically to the cytosol or to the nuclei was observed, thus providing a powerful tool for targeted drug delivery.
Peptoid dendrimers—microwave-assisted solid-phase synthesis and transfection agent evaluation
作者:Juan J. Diaz-Mochon、Mario A. Fara、Rosario M. Sanchez-Martin、Mark Bradley
DOI:10.1016/j.tetlet.2007.11.122
日期:2008.1
Three generations of peptoid-based dendrimers were synthesised by solid-phase methods, using N-Fmoc-N-(6-N'-Fmoc-aminohexyl)glycine as both the initiator core and the monomer unit, which offer an unusual dendrimeric periphery composed of both secondary and primary amines. The third generation compound proved to be an efficient mediator of transfection while displaying minimal cytotoxicity. (C) 2007 Elsevier Ltd. All rights reserved.