Incorporation of a Non‐Natural Arginine Analogue into a Cyclic Peptide Leads to Formation of Positively Charged Nanofibers Capable of Gene Transfection

Abstract

Abstract Functionalization of the tetracationic cyclic peptide (Ka) 4 with a single guanidiniocarbonyl pyrrole (GCP) moiety, a weakly basic but highly efficient arginine analogue, completely alters the self‐assembly properties of the peptide. In contrast to the nonfunctionalized peptide 2 , which does not self‐assemble, GCP‐containing peptide 1 forms cationic nanofibers of micrometer length. These aggregates are efficient gene transfection vectors. DNA binds to their cationic surface and is efficiently delivered into cells.