Identification and evaluation of potent Middle East respiratory syndrome coronavirus (MERS-CoV) 3CLPro inhibitors.
Identifieur interne : 000E21 ( Main/Curation ); précédent : 000E20; suivant : 000E22Identification and evaluation of potent Middle East respiratory syndrome coronavirus (MERS-CoV) 3CLPro inhibitors.
Auteurs : Vathan Kumar [Taïwan] ; Jin Soo Shin [Corée du Sud] ; Jiun-Jie Shie [Taïwan] ; Keun Bon Ku [Corée du Sud] ; Chonsaeng Kim [Corée du Sud] ; Yun Young Go [Corée du Sud] ; Kai-Fa Huang [Taïwan] ; Meehyein Kim [Corée du Sud] ; Po-Huang Liang [Taïwan]Source :
- Antiviral research [ 1872-9096 ] ; 2017.
Descripteurs français
- KwdFr :
- Animaux, Antiviraux (), Antiviraux (isolement et purification), Antiviraux (pharmacologie), Chats, Coronavirus (), Coronavirus du syndrome respiratoire du Moyen-Orient (), Découverte de médicament, Humains, Infections à coronavirus (virologie), Inhibiteurs de protéases (pharmacologie), Peptidomimétiques (), Peptidomimétiques (pharmacologie), Protéines virales, Virus du SRAS ().
- MESH :
- isolement et purification : Antiviraux.
- pharmacologie : Antiviraux, Inhibiteurs de protéases, Peptidomimétiques.
- virologie : Infections à coronavirus.
- Animaux, Antiviraux, Chats, Coronavirus, Coronavirus du syndrome respiratoire du Moyen-Orient, Découverte de médicament, Humains, Peptidomimétiques, Protéines virales, Virus du SRAS.
English descriptors
- KwdEn :
- Animals, Antiviral Agents (chemistry), Antiviral Agents (isolation & purification), Antiviral Agents (pharmacology), Cats, Coronavirus (drug effects), Coronavirus Infections (virology), Drug Discovery, Humans, Middle East Respiratory Syndrome Coronavirus (drug effects), Peptidomimetics (chemistry), Peptidomimetics (pharmacology), Protease Inhibitors (pharmacology), SARS Virus (drug effects), Viral Proteins.
- MESH :
- chemical , chemistry : Antiviral Agents, Peptidomimetics.
- chemical , isolation & purification : Antiviral Agents.
- chemical , pharmacology : Antiviral Agents, Peptidomimetics, Protease Inhibitors.
- drug effects : Coronavirus, Middle East Respiratory Syndrome Coronavirus, SARS Virus.
- virology : Coronavirus Infections.
- Animals, Cats, Drug Discovery, Humans, Viral Proteins.
Abstract
Middle East respiratory syndrome coronavirus (MERS-CoV) causes severe acute respiratory illness with fever, cough and shortness of breath. Up to date, it has resulted in 1826 human infections, including 649 deaths. Analogous to picornavirus 3C protease (3Cpro), 3C-like protease (3CLpro) is critical for initiation of the MERS-CoV replication cycle and is thus regarded as a validated drug target. As presented here, our peptidomimetic inhibitors of enterovirus 3Cpro (6b, 6c and 6d) inhibited 3CLpro of MERS-CoV and severe acute respiratory syndrome coronavirus (SARS-CoV) with IC50 values ranging from 1.7 to 4.7 μM and from 0.2 to 0.7 μM, respectively. In MERS-CoV-infected cells, the inhibitors showed antiviral activity with EC50 values ranging from 0.6 to 1.4 μM, by downregulating the viral protein production in cells as well as reducing secretion of infectious viral particles into culture supernatants. They also suppressed other α- and β-CoVs from human and feline origin. These compounds exhibited good selectivity index (over 70 against MERS-CoV) and could lead to the development of broad-spectrum antiviral drugs against emerging CoVs and picornaviruses.
DOI: 10.1016/j.antiviral.2017.02.007
PubMed: 28216367
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Electronic address: mkim@krict.re.kr.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Korea Research Institute of Chemical Technology, Daejeon</wicri:regionArea><wicri:noRegion>Daejeon</wicri:noRegion></affiliation></author><author><name sortKey="Liang, Po Huang" sort="Liang, Po Huang" uniqKey="Liang P" first="Po-Huang" last="Liang">Po-Huang Liang</name><affiliation wicri:level="1"><nlm:affiliation>Institute of Biological Chemistry, Academia Sinica, Taipei, Taiwan; Institute of Biochemical Sciences, National Taiwan University, Taipei, Taiwan. Electronic address: phliang@gate.sinica.edu.tw.</nlm:affiliation><country xml:lang="fr">Taïwan</country><wicri:regionArea>Institute of Biological Chemistry, Academia Sinica, Taipei, Taiwan; Institute of Biochemical Sciences, National Taiwan University, Taipei</wicri:regionArea><wicri:noRegion>Taipei</wicri:noRegion></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">PubMed</idno><date when="2017">2017</date><idno type="RBID">pubmed:28216367</idno><idno type="pmid">28216367</idno><idno type="doi">10.1016/j.antiviral.2017.02.007</idno><idno type="wicri:Area/PubMed/Corpus">000B51</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Corpus" wicri:corpus="PubMed">000B51</idno><idno type="wicri:Area/PubMed/Curation">000B51</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Curation">000B51</idno><idno type="wicri:Area/PubMed/Checkpoint">000B10</idno><idno type="wicri:explorRef" wicri:stream="Checkpoint" wicri:step="PubMed">000B10</idno><idno type="wicri:Area/Ncbi/Merge">002D69</idno><idno type="wicri:Area/Ncbi/Curation">002D69</idno><idno type="wicri:Area/Ncbi/Checkpoint">002D69</idno><idno type="wicri:Area/Main/Merge">000E23</idno><idno type="wicri:Area/Main/Curation">000E21</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en">Identification and evaluation of potent Middle East respiratory syndrome coronavirus (MERS-CoV) 3CL<sup>Pro</sup> inhibitors.</title><author><name sortKey="Kumar, Vathan" sort="Kumar, Vathan" uniqKey="Kumar V" first="Vathan" last="Kumar">Vathan Kumar</name><affiliation wicri:level="1"><nlm:affiliation>Institute of Biological Chemistry, Academia Sinica, Taipei, Taiwan.</nlm:affiliation><country xml:lang="fr">Taïwan</country><wicri:regionArea>Institute of Biological Chemistry, Academia Sinica, Taipei</wicri:regionArea><wicri:noRegion>Taipei</wicri:noRegion></affiliation></author><author><name sortKey="Shin, Jin Soo" sort="Shin, Jin Soo" uniqKey="Shin J" first="Jin Soo" last="Shin">Jin Soo Shin</name><affiliation wicri:level="1"><nlm:affiliation>Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Korea Research Institute of Chemical Technology, Daejeon</wicri:regionArea><wicri:noRegion>Daejeon</wicri:noRegion></affiliation></author><author><name sortKey="Shie, Jiun Jie" sort="Shie, Jiun Jie" uniqKey="Shie J" first="Jiun-Jie" last="Shie">Jiun-Jie Shie</name><affiliation wicri:level="1"><nlm:affiliation>Institute of Chemistry, Academia Sinica, Taipei, Taiwan.</nlm:affiliation><country xml:lang="fr">Taïwan</country><wicri:regionArea>Institute of Chemistry, Academia Sinica, Taipei</wicri:regionArea><wicri:noRegion>Taipei</wicri:noRegion></affiliation></author><author><name sortKey="Ku, Keun Bon" sort="Ku, Keun Bon" uniqKey="Ku K" first="Keun Bon" last="Ku">Keun Bon Ku</name><affiliation wicri:level="1"><nlm:affiliation>Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Korea Research Institute of Chemical Technology, Daejeon</wicri:regionArea><wicri:noRegion>Daejeon</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Chonsaeng" sort="Kim, Chonsaeng" uniqKey="Kim C" first="Chonsaeng" last="Kim">Chonsaeng Kim</name><affiliation wicri:level="1"><nlm:affiliation>Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Korea Research Institute of Chemical Technology, Daejeon</wicri:regionArea><wicri:noRegion>Daejeon</wicri:noRegion></affiliation></author><author><name sortKey="Go, Yun Young" sort="Go, Yun Young" uniqKey="Go Y" first="Yun Young" last="Go">Yun Young Go</name><affiliation wicri:level="1"><nlm:affiliation>Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Korea Research Institute of Chemical Technology, Daejeon</wicri:regionArea><wicri:noRegion>Daejeon</wicri:noRegion></affiliation></author><author><name sortKey="Huang, Kai Fa" sort="Huang, Kai Fa" uniqKey="Huang K" first="Kai-Fa" last="Huang">Kai-Fa Huang</name><affiliation wicri:level="1"><nlm:affiliation>Institute of Biological Chemistry, Academia Sinica, Taipei, Taiwan.</nlm:affiliation><country xml:lang="fr">Taïwan</country><wicri:regionArea>Institute of Biological Chemistry, Academia Sinica, Taipei</wicri:regionArea><wicri:noRegion>Taipei</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Meehyein" sort="Kim, Meehyein" uniqKey="Kim M" first="Meehyein" last="Kim">Meehyein Kim</name><affiliation wicri:level="1"><nlm:affiliation>Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea. Electronic address: mkim@krict.re.kr.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Korea Research Institute of Chemical Technology, Daejeon</wicri:regionArea><wicri:noRegion>Daejeon</wicri:noRegion></affiliation></author><author><name sortKey="Liang, Po Huang" sort="Liang, Po Huang" uniqKey="Liang P" first="Po-Huang" last="Liang">Po-Huang Liang</name><affiliation wicri:level="1"><nlm:affiliation>Institute of Biological Chemistry, Academia Sinica, Taipei, Taiwan; Institute of Biochemical Sciences, National Taiwan University, Taipei, Taiwan. Electronic address: phliang@gate.sinica.edu.tw.</nlm:affiliation><country xml:lang="fr">Taïwan</country><wicri:regionArea>Institute of Biological Chemistry, Academia Sinica, Taipei, Taiwan; Institute of Biochemical Sciences, National Taiwan University, Taipei</wicri:regionArea><wicri:noRegion>Taipei</wicri:noRegion></affiliation></author></analytic><series><title level="j">Antiviral research</title><idno type="eISSN">1872-9096</idno><imprint><date when="2017" type="published">2017</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Antiviral Agents (chemistry)</term><term>Antiviral Agents (isolation & purification)</term><term>Antiviral Agents (pharmacology)</term><term>Cats</term><term>Coronavirus (drug effects)</term><term>Coronavirus Infections (virology)</term><term>Drug Discovery</term><term>Humans</term><term>Middle East Respiratory Syndrome Coronavirus (drug effects)</term><term>Peptidomimetics (chemistry)</term><term>Peptidomimetics (pharmacology)</term><term>Protease Inhibitors (pharmacology)</term><term>SARS Virus (drug effects)</term><term>Viral Proteins</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Animaux</term><term>Antiviraux ()</term><term>Antiviraux (isolement et purification)</term><term>Antiviraux (pharmacologie)</term><term>Chats</term><term>Coronavirus ()</term><term>Coronavirus du syndrome respiratoire du Moyen-Orient ()</term><term>Découverte de médicament</term><term>Humains</term><term>Infections à coronavirus (virologie)</term><term>Inhibiteurs de protéases (pharmacologie)</term><term>Peptidomimétiques ()</term><term>Peptidomimétiques (pharmacologie)</term><term>Protéines virales</term><term>Virus du SRAS ()</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antiviral Agents</term><term>Peptidomimetics</term></keywords><keywords scheme="MESH" type="chemical" qualifier="isolation & purification" xml:lang="en"><term>Antiviral Agents</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antiviral Agents</term><term>Peptidomimetics</term><term>Protease Inhibitors</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Coronavirus</term><term>Middle East Respiratory Syndrome Coronavirus</term><term>SARS Virus</term></keywords><keywords scheme="MESH" qualifier="isolement et purification" xml:lang="fr"><term>Antiviraux</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antiviraux</term><term>Inhibiteurs de protéases</term><term>Peptidomimétiques</term></keywords><keywords scheme="MESH" qualifier="virologie" xml:lang="fr"><term>Infections à coronavirus</term></keywords><keywords scheme="MESH" qualifier="virology" xml:lang="en"><term>Coronavirus Infections</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Cats</term><term>Drug Discovery</term><term>Humans</term><term>Viral Proteins</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Animaux</term><term>Antiviraux</term><term>Chats</term><term>Coronavirus</term><term>Coronavirus du syndrome respiratoire du Moyen-Orient</term><term>Découverte de médicament</term><term>Humains</term><term>Peptidomimétiques</term><term>Protéines virales</term><term>Virus du SRAS</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Middle East respiratory syndrome coronavirus (MERS-CoV) causes severe acute respiratory illness with fever, cough and shortness of breath. Up to date, it has resulted in 1826 human infections, including 649 deaths. Analogous to picornavirus 3C protease (3C<sup>pro</sup>), 3C-like protease (3CL<sup>pro</sup>) is critical for initiation of the MERS-CoV replication cycle and is thus regarded as a validated drug target. As presented here, our peptidomimetic inhibitors of enterovirus 3C<sup>pro</sup> (6b, 6c and 6d) inhibited 3CL<sup>pro</sup> of MERS-CoV and severe acute respiratory syndrome coronavirus (SARS-CoV) with IC<sub>50</sub> values ranging from 1.7 to 4.7 μM and from 0.2 to 0.7 μM, respectively. In MERS-CoV-infected cells, the inhibitors showed antiviral activity with EC<sub>50</sub> values ranging from 0.6 to 1.4 μM, by downregulating the viral protein production in cells as well as reducing secretion of infectious viral particles into culture supernatants. They also suppressed other α- and β-CoVs from human and feline origin. These compounds exhibited good selectivity index (over 70 against MERS-CoV) and could lead to the development of broad-spectrum antiviral drugs against emerging CoVs and picornaviruses.</div></front></TEI></record>Pour manipuler ce document sous Unix (Dilib)
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