Identification of a short ACE2-derived stapled peptide targeting the SARS-CoV-2 spike protein.
Eur J Med Chem
; 249: 115118, 2023 Mar 05.
Article
in English
| MEDLINE | ID: covidwho-2178286
ABSTRACT
The design and synthesis of a series of peptide derivatives based on a short ACE2 α-helix 1 epitope and subsequent [i - i+4] stapling of the secondary structure resulted in the identification of a 9-mer peptide capable to compete with recombinant ACE2 towards Spike RBD in the micromolar range. Specifically, SARS-CoV-2 Spike inhibitor screening based on colorimetric ELISA assay and structural studies by circular dichroism showed the ring-closing metathesis cyclization being capable to stabilize the helical structure of the 9-mer 34HEAEDLFYQ42 epitope better than the triazole stapling via click chemistry. MD simulations showed the stapled peptide being able not only to bind the Spike RBD, sterically interfering with ACE2, but also showing higher affinity to the target as compared to parent epitope.
Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Spike Glycoprotein, Coronavirus
/
COVID-19
Type of study:
Diagnostic study
Limits:
Humans
Language:
English
Journal:
Eur J Med Chem
Year:
2023
Document Type:
Article
Affiliation country:
J.ejmech.2023.115118
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