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@ARTICLE{Mastalipour:1046365,
author = {Mastalipour, Mohammadamin and Gering, Ian and Coronado,
Mônika Aparecida and González, Jorge Enrique Hernández
and Willbold, Dieter and Eberle, Raphael Josef},
title = {{N}ovel peptide inhibitor for the {C}hikungunya virus
ns{P}2 protease: {I}dentification and characterization},
journal = {Current research in microbial sciences},
volume = {8},
issn = {2666-5174},
address = {Amsterdam},
publisher = {Elsevier B.V.},
reportid = {FZJ-2025-03793},
pages = {100376 -},
year = {2025},
abstract = {Chikungunya virus (CHIKV) is an emerging pathogen affecting
populations worldwide, with rapidly increasing infection
rates. CHIKV, an arbovirus of the alphavirus genus, is
predominantly found in tropical regions and transmitted by
Aedes mosquitoes. Climate change has accelerated the global
spread of these vectors, leading to outbreaks in
non-tropical regions, including parts of Europe. The absence
of antiviral therapies and the potential for co-infections
with other viruses make CHIKV a significant public health
concern. CHIKV replication relies on nsP2 cysteine protease
activity to cleave its viral polyprotein into functional
nonstructural and structural proteins. Targeting the nsP2
protease represents a promising strategy for antiviral
therapy development. In this study, phage display was used
to screen a library of peptides for potential binders of the
target protease. Biophysical and biochemical analyses of the
identified peptides assessed their inhibitory potential.
Among the six identified peptides (named as P1–P6), four
demonstrated inhibitory effects on the nsP2 protease
(nsP2pro). Peptide P1 exhibited the strongest inhibitory
effect, with a half-maximal inhibitory concentration (IC50)
of 4.6 ± 1.9 µM, and a low cytotoxicity. The secondary
structure analysis through CD spectroscopy and homology
modelling revealed that P1 adopts an alpha-helical
conformation. Finally, molecular dynamics simulations
enabled us to investigate the dynamics of the nsP2pro active
site and molecular docking was employed to predict the
orthosteric binding mode of P1, providing insights into
protein-peptide interaction. These findings underscore the
potential of peptide P1 as a lead compound for further
investigation in the context of CHIKV research.},
cin = {IBI-7},
ddc = {570},
cid = {I:(DE-Juel1)IBI-7-20200312},
pnm = {5241 - Molecular Information Processing in Cellular Systems
(POF4-524)},
pid = {G:(DE-HGF)POF4-5241},
typ = {PUB:(DE-HGF)16},
pubmed = {40165933},
UT = {WOS:001448662000001},
doi = {10.1016/j.crmicr.2025.100376},
url = {https://juser.fz-juelich.de/record/1046365},
}