Bis‐Lactam Peptide [ i , i + 4]‐Stapling

of main observation and conclusion Even though the bis-lactam peptide stapling with the [i, i + 7] and the [i, i + 11] systems has been known to be able to afford % alpha-helicity values up to 100% (25 degrees C), the performance of the bis-lactam peptide stapling with the [i, i + 4] system in current literature has been mediocre (% alpha-helicity <= 40%, 25 degrees C). In the current study, we found that high % alpha-helicity is also obtainable with the bis-lactam [i, i + 4]-stapling by demonstrating with our model peptide sequence that the bis-lactam [i, i + 4]-stapling with N-epsilon-para-phenylenediacetyl-lysine was able to afford a % alpha-helicity value of similar to 64.1% (25 degrees C). Therefore, the bis-lactam [i, i + 4]-stapling could also be an efficacious peptide stapling mode that can be employed for biomedical applications.