Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors.
Identifieur interne : 003E37 ( Main/Exploration ); précédent : 003E36; suivant : 003E38Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors.
Auteurs : Lu Zhou [République populaire de Chine] ; Ying Liu ; Weilin Zhang ; Ping Wei ; Changkang Huang ; Jianfeng Pei ; Yaxia Yuan ; Luhua LaiSource :
- Journal of medicinal chemistry [ 0022-2623 ] ; 2006.
Descripteurs français
- KwdFr :
- MESH :
- analogues et dérivés : Isatine.
- antagonistes et inhibiteurs : Protéines virales.
- enzymologie : Virus du SRAS.
- synthèse chimique : Isatine.
- Cysteine endopeptidases, Humains, Isatine, Modèles moléculaires, Protéines virales.
English descriptors
- KwdEn :
- MESH :
- chemical , analogs & derivatives : Isatin.
- chemical , antagonists & inhibitors : Viral Proteins.
- chemical , chemical synthesis : Isatin.
- chemical , chemistry : Cysteine Endopeptidases, Isatin, Viral Proteins.
- enzymology : SARS Virus.
- Humans, Models, Molecular.
Abstract
A series of isatin derivatives were synthesized and tested against SARS CoV 3C-like protease. Substitutions at the N-1 and C-5 positions were examined to elucidate the differences in substrate binding sites of the rhinovirus 3C protease and SARS CoV 3C-like protease. Compound 5f shows significant inhibition with an IC(50) of 0.37 microM. Further study showed that, unlike the irreversible covalent binding of isatin derivatives to human rhinovirus 3C protease, the compounds tested in this study are all noncovalent reversible inhibitors.
DOI: 10.1021/jm0602357
PubMed: 16759084
Affiliations:
Links toward previous steps (curation, corpus...)
- to stream PubMed, to step Corpus: 002214
- to stream PubMed, to step Curation: 002214
- to stream PubMed, to step Checkpoint: 002127
- to stream Ncbi, to step Merge: 001524
- to stream Ncbi, to step Curation: 001524
- to stream Ncbi, to step Checkpoint: 001524
- to stream Main, to step Merge: 004019
- to stream Main, to step Curation: 003E37
Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors.</title><author><name sortKey="Zhou, Lu" sort="Zhou, Lu" uniqKey="Zhou L" first="Lu" last="Zhou">Lu Zhou</name><affiliation wicri:level="4"><nlm:affiliation>State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871</wicri:regionArea><placeName><settlement type="city">Pékin</settlement></placeName><orgName type="university">Université de Pékin</orgName><placeName><settlement type="city">Pékin</settlement><region type="capitale">Pékin</region></placeName></affiliation></author><author><name sortKey="Liu, Ying" sort="Liu, Ying" uniqKey="Liu Y" first="Ying" last="Liu">Ying Liu</name></author><author><name sortKey="Zhang, Weilin" sort="Zhang, Weilin" uniqKey="Zhang W" first="Weilin" last="Zhang">Weilin Zhang</name></author><author><name sortKey="Wei, Ping" sort="Wei, Ping" uniqKey="Wei P" first="Ping" last="Wei">Ping Wei</name></author><author><name sortKey="Huang, Changkang" sort="Huang, Changkang" uniqKey="Huang C" first="Changkang" last="Huang">Changkang Huang</name></author><author><name sortKey="Pei, Jianfeng" sort="Pei, Jianfeng" uniqKey="Pei J" first="Jianfeng" last="Pei">Jianfeng Pei</name></author><author><name sortKey="Yuan, Yaxia" sort="Yuan, Yaxia" uniqKey="Yuan Y" first="Yaxia" last="Yuan">Yaxia Yuan</name></author><author><name sortKey="Lai, Luhua" sort="Lai, Luhua" uniqKey="Lai L" first="Luhua" last="Lai">Luhua Lai</name></author></titleStmt><publicationStmt><idno type="wicri:source">PubMed</idno><date when="2006">2006</date><idno type="RBID">pubmed:16759084</idno><idno type="pmid">16759084</idno><idno type="doi">10.1021/jm0602357</idno><idno type="wicri:Area/PubMed/Corpus">002214</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Corpus" wicri:corpus="PubMed">002214</idno><idno type="wicri:Area/PubMed/Curation">002214</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Curation">002214</idno><idno type="wicri:Area/PubMed/Checkpoint">002127</idno><idno type="wicri:explorRef" wicri:stream="Checkpoint" wicri:step="PubMed">002127</idno><idno type="wicri:Area/Ncbi/Merge">001524</idno><idno type="wicri:Area/Ncbi/Curation">001524</idno><idno type="wicri:Area/Ncbi/Checkpoint">001524</idno><idno type="wicri:doubleKey">0022-2623:2006:Zhou L:isatin:compounds:as</idno><idno type="wicri:Area/Main/Merge">004019</idno><idno type="wicri:Area/Main/Curation">003E37</idno><idno type="wicri:Area/Main/Exploration">003E37</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en">Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors.</title><author><name sortKey="Zhou, Lu" sort="Zhou, Lu" uniqKey="Zhou L" first="Lu" last="Zhou">Lu Zhou</name><affiliation wicri:level="4"><nlm:affiliation>State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871</wicri:regionArea><placeName><settlement type="city">Pékin</settlement></placeName><orgName type="university">Université de Pékin</orgName><placeName><settlement type="city">Pékin</settlement><region type="capitale">Pékin</region></placeName></affiliation></author><author><name sortKey="Liu, Ying" sort="Liu, Ying" uniqKey="Liu Y" first="Ying" last="Liu">Ying Liu</name></author><author><name sortKey="Zhang, Weilin" sort="Zhang, Weilin" uniqKey="Zhang W" first="Weilin" last="Zhang">Weilin Zhang</name></author><author><name sortKey="Wei, Ping" sort="Wei, Ping" uniqKey="Wei P" first="Ping" last="Wei">Ping Wei</name></author><author><name sortKey="Huang, Changkang" sort="Huang, Changkang" uniqKey="Huang C" first="Changkang" last="Huang">Changkang Huang</name></author><author><name sortKey="Pei, Jianfeng" sort="Pei, Jianfeng" uniqKey="Pei J" first="Jianfeng" last="Pei">Jianfeng Pei</name></author><author><name sortKey="Yuan, Yaxia" sort="Yuan, Yaxia" uniqKey="Yuan Y" first="Yaxia" last="Yuan">Yaxia Yuan</name></author><author><name sortKey="Lai, Luhua" sort="Lai, Luhua" uniqKey="Lai L" first="Luhua" last="Lai">Luhua Lai</name></author></analytic><series><title level="j">Journal of medicinal chemistry</title><idno type="ISSN">0022-2623</idno><imprint><date when="2006" type="published">2006</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Cysteine Endopeptidases (chemistry)</term><term>Humans</term><term>Isatin (analogs & derivatives)</term><term>Isatin (chemical synthesis)</term><term>Isatin (chemistry)</term><term>Models, Molecular</term><term>SARS Virus (enzymology)</term><term>Viral Proteins (antagonists & inhibitors)</term><term>Viral Proteins (chemistry)</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Cysteine endopeptidases ()</term><term>Humains</term><term>Isatine ()</term><term>Isatine (analogues et dérivés)</term><term>Isatine (synthèse chimique)</term><term>Modèles moléculaires</term><term>Protéines virales ()</term><term>Protéines virales (antagonistes et inhibiteurs)</term><term>Virus du SRAS (enzymologie)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analogs & derivatives" xml:lang="en"><term>Isatin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>Viral Proteins</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Isatin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Cysteine Endopeptidases</term><term>Isatin</term><term>Viral Proteins</term></keywords><keywords scheme="MESH" qualifier="analogues et dérivés" xml:lang="fr"><term>Isatine</term></keywords><keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr"><term>Protéines virales</term></keywords><keywords scheme="MESH" qualifier="enzymologie" xml:lang="fr"><term>Virus du SRAS</term></keywords><keywords scheme="MESH" qualifier="enzymology" xml:lang="en"><term>SARS Virus</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Isatine</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Humans</term><term>Models, Molecular</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Cysteine endopeptidases</term><term>Humains</term><term>Isatine</term><term>Modèles moléculaires</term><term>Protéines virales</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">A series of isatin derivatives were synthesized and tested against SARS CoV 3C-like protease. Substitutions at the N-1 and C-5 positions were examined to elucidate the differences in substrate binding sites of the rhinovirus 3C protease and SARS CoV 3C-like protease. Compound 5f shows significant inhibition with an IC(50) of 0.37 microM. Further study showed that, unlike the irreversible covalent binding of isatin derivatives to human rhinovirus 3C protease, the compounds tested in this study are all noncovalent reversible inhibitors.</div></front></TEI><affiliations><list><country><li>République populaire de Chine</li></country><region><li>Pékin</li></region><settlement><li>Pékin</li></settlement><orgName><li>Université de Pékin</li></orgName></list><tree><noCountry><name sortKey="Huang, Changkang" sort="Huang, Changkang" uniqKey="Huang C" first="Changkang" last="Huang">Changkang Huang</name><name sortKey="Lai, Luhua" sort="Lai, Luhua" uniqKey="Lai L" first="Luhua" last="Lai">Luhua Lai</name><name sortKey="Liu, Ying" sort="Liu, Ying" uniqKey="Liu Y" first="Ying" last="Liu">Ying Liu</name><name sortKey="Pei, Jianfeng" sort="Pei, Jianfeng" uniqKey="Pei J" first="Jianfeng" last="Pei">Jianfeng Pei</name><name sortKey="Wei, Ping" sort="Wei, Ping" uniqKey="Wei P" first="Ping" last="Wei">Ping Wei</name><name sortKey="Yuan, Yaxia" sort="Yuan, Yaxia" uniqKey="Yuan Y" first="Yaxia" last="Yuan">Yaxia Yuan</name><name sortKey="Zhang, Weilin" sort="Zhang, Weilin" uniqKey="Zhang W" first="Weilin" last="Zhang">Weilin Zhang</name></noCountry><country name="République populaire de Chine"><noRegion><name sortKey="Zhou, Lu" sort="Zhou, Lu" uniqKey="Zhou L" first="Lu" last="Zhou">Lu Zhou</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Sante/explor/SrasV1/Data/Main/Exploration
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 003E37 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 003E37 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien
|wiki= Sante
|area= SrasV1
|flux= Main
|étape= Exploration
|type= RBID
|clé= pubmed:16759084
|texte= Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors.
}}
Pour générer des pages wiki
HfdIndexSelect -h $EXPLOR_AREA/Data/Main/Exploration/RBID.i -Sk "pubmed:16759084" \
| HfdSelect -Kh $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd \
| NlmPubMed2Wicri -a SrasV1
| This area was generated with Dilib version V0.6.33. |  |