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Individual and common inhibitors of coronavirus and picornavirus main proteases

Identifieur interne : 000D14 ( Pmc/Checkpoint ); précédent : 000D13; suivant : 000D15

Individual and common inhibitors of coronavirus and picornavirus main proteases

Auteurs : Chih-Jung Kuo ; Hun-Ge Liu ; Yueh-Kuei Lo ; Churl-Min Seong ; Kee-In Lee ; Young-Sik Jung ; Po-Huang Liang

Source :

RBID : PMC:7094298

Abstract

Picornaviruses (PV) and coronaviruses (CoV) are positive‐stranded RNA viruses which infect millions of people worldwide each year, resulting in a wide range of clinical outcomes. As reported in this study, using high throughput screening against ∼6800 small molecules, we have identified several novel inhibitors of SARS‐CoV 3CLpro with IC50 of low μM. Interestingly, one of them equally inhibited both 3Cpro and 3CLpro from PV and CoV, respectively. Using computer modeling, the structural features of these compounds as individual and common protease inhibitors were elucidated to enhance our knowledge for developing anti‐viral agents against PV and CoV.


Url:
DOI: 10.1016/j.febslet.2008.12.059
PubMed: 19166843
PubMed Central: 7094298


Affiliations:


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PMC:7094298

Le document en format XML

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<p>Picornaviruses (PV) and coronaviruses (CoV) are positive‐stranded RNA viruses which infect millions of people worldwide each year, resulting in a wide range of clinical outcomes. As reported in this study, using high throughput screening against ∼6800 small molecules, we have identified several novel inhibitors of SARS‐CoV 3CL
<sup>pro</sup>
with IC
<sub>50</sub>
of low μM. Interestingly, one of them equally inhibited both 3C
<sup>pro</sup>
and 3CL
<sup>pro</sup>
from PV and CoV, respectively. Using computer modeling, the structural features of these compounds as individual and common protease inhibitors were elucidated to enhance our knowledge for developing anti‐viral agents against PV and CoV.</p>
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<name>
<surname>Kuo</surname>
<given-names>Chih-Jung</given-names>
</name>
<xref ref-type="aff" rid="feb2s0014579309000167-aff-aff1">
<sup>1</sup>
</xref>
<xref ref-type="aff" rid="feb2s0014579309000167-aff-aff2">
<sup>2</sup>
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<surname>Liu</surname>
<given-names>Hun-Ge</given-names>
</name>
<xref ref-type="aff" rid="feb2s0014579309000167-aff-aff1">
<sup>1</sup>
</xref>
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<surname>Lo</surname>
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<sup>1</sup>
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<sup>3</sup>
</xref>
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<name>
<surname>Lee</surname>
<given-names>Kee-In</given-names>
</name>
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<sup>3</sup>
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<sup>3</sup>
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<email>ysjung@krict.re.kr</email>
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<name>
<surname>Liang</surname>
<given-names>Po-Huang</given-names>
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<sup>1</sup>
</xref>
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<sup>2</sup>
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<email>phliang@gate.sinica.edu.tw</email>
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<sup>1</sup>
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Institute of Biological Chemistry, Academia Sinica, Taipei 11529, Taiwan, ROC</aff>
<aff id="feb2s0014579309000167-aff-aff2">
<label>
<sup>2</sup>
</label>
Taiwan International Graduate Program, Academia Sinica, Taipei 11529, Taiwan</aff>
<aff id="feb2s0014579309000167-aff-aff3">
<label>
<sup>3</sup>
</label>
Korea Research Institute of Chemical Technology, Daejeon 305-606, Republic of Korea</aff>
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<label>*</label>
Corresponding authors. Address: Institute of Biological Chemistry, Academia Sinica, Taipei 11529, Taiwan, ROC. Fax: +886 2 2788 9759.</corresp>
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<day>04</day>
<month>2</month>
<year>2009</year>
</pub-date>
<pub-date pub-type="epub">
<day>21</day>
<month>1</month>
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<volume>583</volume>
<issue>3</issue>
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<fpage>549</fpage>
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<date date-type="rev-recd">
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<year>2008</year>
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<pmc-comment> © 2015 Federation of European Biochemical Societies </pmc-comment>
<copyright-statement content-type="article-copyright">FEBS Letters 583 (2009) 1873-3468 © 2015 Federation of European Biochemical Societies</copyright-statement>
<license>
<license-p>This article is being made freely available through PubMed Central as part of the COVID-19 public health emergency response. It can be used for unrestricted research re-use and analysis in any form or by any means with acknowledgement of the original source, for the duration of the public health emergency.</license-p>
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<abstract>
<p>Picornaviruses (PV) and coronaviruses (CoV) are positive‐stranded RNA viruses which infect millions of people worldwide each year, resulting in a wide range of clinical outcomes. As reported in this study, using high throughput screening against ∼6800 small molecules, we have identified several novel inhibitors of SARS‐CoV 3CL
<sup>pro</sup>
with IC
<sub>50</sub>
of low μM. Interestingly, one of them equally inhibited both 3C
<sup>pro</sup>
and 3CL
<sup>pro</sup>
from PV and CoV, respectively. Using computer modeling, the structural features of these compounds as individual and common protease inhibitors were elucidated to enhance our knowledge for developing anti‐viral agents against PV and CoV.</p>
</abstract>
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<string-name>
<surname>Kuo</surname>
<given-names>Chih-Jung</given-names>
</string-name>
,
<string-name>
<surname>Liu</surname>
<given-names>Hun-Ge</given-names>
</string-name>
,
<string-name>
<surname>Lo</surname>
<given-names>Yueh-Kuei</given-names>
</string-name>
,
<string-name>
<surname>Seong</surname>
<given-names>Churl-Min</given-names>
</string-name>
,
<string-name>
<surname>Lee</surname>
<given-names>Kee-In</given-names>
</string-name>
,
<string-name>
<surname>Jung</surname>
<given-names>Young-Sik</given-names>
</string-name>
and
<string-name>
<surname>Liang</surname>
<given-names>Po-Huang</given-names>
</string-name>
(
<year>2009</year>
),
<article-title>Individual and common inhibitors of coronavirus and picornavirus main proteases</article-title>
,
<source xml:lang="en">FEBS Letters</source>
,
<volume>583</volume>
, doi: 10.1016/j.febslet.2008.12.059</mixed-citation>
</p>
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<name sortKey="Jung, Young Sik" sort="Jung, Young Sik" uniqKey="Jung Y" first="Young-Sik" last="Jung">Young-Sik Jung</name>
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<name sortKey="Lee, Kee In" sort="Lee, Kee In" uniqKey="Lee K" first="Kee-In" last="Lee">Kee-In Lee</name>
<name sortKey="Liang, Po Huang" sort="Liang, Po Huang" uniqKey="Liang P" first="Po-Huang" last="Liang">Po-Huang Liang</name>
<name sortKey="Liu, Hun Ge" sort="Liu, Hun Ge" uniqKey="Liu H" first="Hun-Ge" last="Liu">Hun-Ge Liu</name>
<name sortKey="Lo, Yueh Kuei" sort="Lo, Yueh Kuei" uniqKey="Lo Y" first="Yueh-Kuei" last="Lo">Yueh-Kuei Lo</name>
<name sortKey="Seong, Churl Min" sort="Seong, Churl Min" uniqKey="Seong C" first="Churl-Min" last="Seong">Churl-Min Seong</name>
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