New Methods for Construction and Modification of Complex Peptides

 

 

 

 

 

Peptides have emerged as a powerful platform for exploring the biorelevant chemical space that bridges the gap between small molecules and biologics. However, when compared to the state-of-the-art techniques in small molecule synthesis, chemists face formidable challenges in customizing the three-dimensional structures and physiochemical properties of cyclic peptides. In this talk, I will discuss our recent research focused on diverse chemical strategies aimed at synthesizing peptide macrocycles with distinct structure features and a high-throughput capacity: 1) Construction of “cyclophane-braced” peptide macrocycles via palladium-catalyzed intramolecular arylation chemistry; 2) Stapling of unprotected native peptides with simple aldehyde reagents. These methodologies hold promises for expanding the repertoire of cyclic peptides and enhancing their potential applications in drug discovery and therapeutic development.