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Schematic illustration of the principle of using selective N-methylation of small cyclic peptides to improve membrane permeability. Exposed amides of cyclic peptides, as shown in red circles in the top peptide, are thought to reduce or prevent membrane permeability. Selective N-methylation of the amides (shown in boxes on the bottom peptide) can increase membrane permeability of the peptide by masking the exposed NH moieties.
