Synthesis of In-Tether Chiral Center Peptides and Their Biophysical Properties Study

The majority of protein-protein interactions (PPIs) involve α-helices and are usually untreatable with small molecules due to their large interaction areas and shallow surfaces. Therefore, the development of constrained peptides that can modulate PPIs by enhancing the helicity of short peptides is important. Many strategies have been developed and successfully applied. Early approaches to stabilize an α-helix involved both polar and physiological labile linkages, such as disulfide bonds and lactam bridges. A significant advance in this field was made by applying ring-closing metathesis to construct constrained peptides.