Stearylated arginine-rich peptides: A new class of transfection systems

Membrane-permeable arginine-rich peptides, such as HIV-1 Tat-(48-60), HIV-1 Rev-(34-50), and flock house virus (FHV) coat-(35-49), have been shown to possess the ability to transfect COS-7 cells with luciferase-coding plasmid as efficiently as polyarginine (MW 5000-15000) and polylysine (MW 9800). N ot only these virus-derived cationic peptides but also oligoarginines of 4- 16 residues were found to be able to transfect cells. In the case of the Ta t, FHV, and octaarginine peptides, N-terminal stearylation of the peptides increases the transfection efficiency by approximately 100 times to reach t he same order of magnitude as that of LipofectAMINE, one of the most effici ent commercially available transfection agents. Also, a certain correlation was observed between the transfection efficiency of stearyl-(Arg)(n) pepti des (stearyl-R-n: n = 4, 8, 12, 16) and the membrane permeability of the co rresponding (Arg)(n) peptides (R-n).