Quantitative Evaluation of the Relative Cell Permeability of Peptoids and Peptides

摘要

We evaluated quantitatively the relative cell permeability of analogous peptoids and peptides using a reporter gene-based assay in vivo. Generally, peptoids were much more cell permeable than the corresponding peptides. This suggests that the attachment of side chains to the amide backbone nitrogen atom instead of the α-carbon, which eliminates the polar N-H bond of the peptide, increases the lipophilicity of the molecule and promotes movement across the cell membrane. Finally, this should be a general method with which to compare the cell permeability of any class of peptidomimetics with the corresponding peptides.