Design and characterization of novel SARS-CoV-2 fusion inhibitors with N-terminally extended HR2 peptides.

ABSTRACT: Development of potent and broad-spectrum antivirals against SARS-CoV-2 remains one of top priorities, especially in the case of that current vaccines cannot effectively prevent viral transmission. We previously generated a group of fusion-inhibitory lipopeptides, with one formulation being evaluated under clinical trials. In this study, we dedicated to characterize the extended N-terminal motif (residues 1161-1168) of the so-called spike (S) heptad repeat 2 (HR2) region. Alanine scanning analysis of this motif verified its critical roles in S protein-mediated cell-cell fusion. Using a panel of HR2 peptides with the N-terminal extensions, we identified a peptide termed P40, which contained four extended N-terminal residues (VDLG) and exhibited improved binding and antiviral activities, wher

SUBMITTER: Hu Y 

PROVIDER: S-EPMC9977133 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature