Discovery of New Potent anti-MERS CoV Fusion Inhibitors.
Front Pharmacol
; 12: 685161, 2021.
Article
in English
| MEDLINE | ID: covidwho-1274604
ABSTRACT
Middle East respiratory syndrome coronavirus (MERS-CoV), capable of zoonotic transmission, has been associated with emerging viral pneumonia in humans. In this study, a set of highly potent peptides were designed to prevent MERS-CoV fusion through competition with heptad repeat domain 2 (HR2) at its HR1 binding site. We designed eleven peptides with stronger estimated HR1 binding affinities than the wild-type peptide to prevent viral fusion with the cell membrane. Eight peptides showed strong inhibition of spike-mediated MERS-CoV cell-cell fusion with IC50 values in the nanomolar range (0.25-2.3 µM). Peptides #4-6 inhibited 95-98.3% of MERS-CoV plaque formation. Notably, peptide four showed strong inhibition of MERS-CoV plaques formation with EC50 = 0.302 µM. All peptides demonstrated safe profiles without cytotoxicity up to a concentration of 10 µM, and this cellular safety, combined with their anti-MERS-CoV antiviral activity, indicate all peptides can be regarded as potential promising antiviral agents.
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Language:
English
Journal:
Front Pharmacol
Year:
2021
Document Type:
Article
Affiliation country:
Fphar.2021.685161
Similar
MEDLINE
...
LILACS
LIS