Discovery of Cyclic Peptide Inhibitors Targeting PD-L1 for Cancer Immunotherapy.

ABSTRACT: Blockade of the interaction between programmed cell death ligand-1 (PD-L1) and its receptor PD-1 has shown great success in cancer immunotherapy. Peptides possess unique characteristics that give them significant advantages as immune checkpoint inhibitors. However, unfavorable physicochemical properties and proteolytic stability profiles limit the translation of bioactive peptides as therapeutic agents. Studies have revealed that cyclization improves the biological activity and stability of linear peptides. In this study, we report the use of macrocyclization scanning for the discovery of cyclic anti-PD-L1 peptides with improved bioactivity. The cyclic peptides demonstrated up to a 34-fold improvement in the PD-1/PD-L1 blocking activity and significant in vivo anti-tumor activity. Our resu

SUBMITTER: Fetse J 

PROVIDER: S-EPMC10671706 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature