Advantages of N-methylation
N-methylation (and N-alkylation more broadly) increases steric hindrance around the peptide bond, reducing the peptide’s entropy and increasing affinity and selectivity. This modification also confers protease resistance, and the disruption of hydrogen bonds can improve bioavailability.
Access to N-methylated amino acids adds another layer of combinatorial diversity to peptides and small molecules, expanding the chemical space you can access for drug discovery.
Incorporate N-methyl amino acids into your workflow to:
- improve protease stability
- improve binding affinity & specificity
- alter molecular flexibility
- identify key interactions with N-methyl scanning
- improve membrane permeability
- improve oral bioavailability