Cyclopeptides have emerged as promising candidates for drug development. However, owing to the scarcity of efficient cyclization strategies for natural peptides, the development of diverse cyclopeptides remains a formidable challenge. In this study, a variety of macrocyclic peptides featuring (thio)urea bridges are dev...
Peptide stapling exerts profound effects on key peptide properties, including metabolic stability, cell membrane permeability, and conformational constraint. Herein, we report a mild and efficient 2,4-dichloro-1,3,5-triazine-mediated stapling strategy for the selective cross-linking of lysine side-chain amines. This ap...