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A covalent chemical probe for Chikungunya nsP2 cysteine protease with antialphaviral activity and proteome-wide selectivity
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A covalent chemical probe for Chikungunya nsP2 cysteine protease with antialphaviral activity and proteome-wide selectivity
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Journal Article
A covalent chemical probe for Chikungunya nsP2 cysteine protease with antialphaviral activity and proteome-wide selectivity
2025
Overview
Chikungunya
is a mosquito-borne viral disease that causes fever and severe joint pain for which there is no direct acting drug treatments. Vinyl sulfone SGC-NSP2PRO-1 (
3
) was identified as a potent inhibitor of the nsP2 cysteine protease (nsP2pro) that reduced viral titer against infectious isolates of
Chikungunya
and other alphaviruses. The covalent warhead in
3
captured the active site C478 and inactivated nsP2pro with a
k
inact
/
K
i
ratio of 5950 M
–1
s
–1
. The vinyl sulfone
3
was inactive across a panel of 23 other cysteine proteases and demonstrated remarkable proteome-wide selectivity by two chemoproteomic methods. A negative control analog SGC-NSP2PRO-1N (
4
) retained the isoxazole core and covalent warhead but demonstrated > 100-fold decrease in enzyme inhibition. Both
3
and
4
were stable across a wide range of pH in solution and upon prolonged storage as solids. Vinyl sulfone
3
and its negative control
4
will find utility as high-quality chemical probes to study the role of the nsP2pro in cellular studies of alphaviral replication and virulence.
Publisher
Nature Publishing Group UK,Nature Publishing Group,Nature Portfolio
Subject
/ Animals
/ Antiviral Agents - chemistry
/ Antiviral Agents - pharmacology
/ Chikungunya Fever - drug therapy
/ Chikungunya Fever - virology
/ Chikungunya virus - drug effects
/ Chikungunya virus - enzymology
/ Cysteine
/ Cysteine Proteases - chemistry
/ Cysteine Proteases - metabolism
/ Cysteine Proteinase Inhibitors - chemistry
/ Cysteine Proteinase Inhibitors - pharmacology
/ Enzymes
/ Genomics
/ Humanities and Social Sciences
/ Humans
/ Molecular Probes - chemistry
/ Molecular Probes - pharmacology
/ Pharmacy
/ Science
/ Viruses
