A facile strategy for the construction of a phage display cyclic peptide library for the selection of functional macrocycles.

ABSTRACT: Cyclic peptides represent invaluable scaffolds in biological affinity, providing diverse collections for discovering functional molecules targeting challenging biological entities and protein-protein interactions. The field increasingly focuses on developing cyclization strategies and chemically modified combinatorial libraries in conjunction with M13 phage display, to identify macrocyclic peptide inhibitors for traditionally challenging targets. Here, we introduce a cyclization strategy utilizing ortho-phthalaldehyde (OPA) for the discovery of active macrocycles characterized by asymmetric scaffolds with side-chain cyclization. Through this approach, aldehyde groups attached to free molecules sequentially attack the ε-amine of lysine and the thiol of cysteine, facilitating the rapi

SUBMITTER: Xiang H 

PROVIDER: S-EPMC11290325 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature