Peptoidic Amino- and Guanidinium-carrier Systems: Targeted Drug Delivery into the Cell Cytosol or the Nucleus

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.