Evaluation of peptide-aldehyde inhibitors using R188I mutant of SARS 3CL protease as a proteolysis-resistant mutant
Identifieur interne : 003202 ( Main/Merge ); précédent : 003201; suivant : 003203Evaluation of peptide-aldehyde inhibitors using R188I mutant of SARS 3CL protease as a proteolysis-resistant mutant
Auteurs : Kenichi Akaji [Japon] ; Hiroyuki Konno [Japon] ; Mari Onozuka [Japon] ; Ayumi Makino [Japon] ; Hiroyuki Saito [Japon] ; Kazuto Nosaka [Japon]Source :
- Bioorganic & Medicinal Chemistry [ 0968-0896 ] ; 2008.
Descripteurs français
- KwdFr :
- Aldéhydes (pharmacologie), Aldéhydes (synthèse chimique), Conformation des protéines, Cysteine endopeptidases (génétique), Cysteine endopeptidases (métabolisme), Données de séquences moléculaires, Humains, Hydrolyse, Inhibiteurs de protéases (pharmacologie), Inhibiteurs de protéases (synthèse chimique), Maturation post-traductionnelle des protéines, Modèles moléculaires, Mutation (génétique), Protéines virales (antagonistes et inhibiteurs), Protéines virales (génétique), Protéines virales (métabolisme), Sites de fixation, Spectrométrie de masse MALDI, Spécificité du substrat, Structure moléculaire, Syndrome respiratoire aigu sévère (génétique), Séquence d'acides aminés, Virus du SRAS (enzymologie), Virus du SRAS (génétique), Virus du SRAS (métabolisme).
- MESH :
- antagonistes et inhibiteurs : Protéines virales.
- enzymologie : Virus du SRAS.
- génétique : Cysteine endopeptidases, Mutation, Protéines virales, Syndrome respiratoire aigu sévère, Virus du SRAS.
- métabolisme : Cysteine endopeptidases, Protéines virales, Virus du SRAS.
- pharmacologie : Aldéhydes, Inhibiteurs de protéases.
- synthèse chimique : Aldéhydes, Inhibiteurs de protéases.
- Conformation des protéines, Données de séquences moléculaires, Humains, Hydrolyse, Maturation post-traductionnelle des protéines, Modèles moléculaires, Sites de fixation, Spectrométrie de masse MALDI, Spécificité du substrat, Structure moléculaire, Séquence d'acides aminés.
English descriptors
- KwdEn :
- Aldehydes (chemical synthesis), Aldehydes (pharmacology), Amino Acid Sequence, Binding Sites, Cysteine Endopeptidases (genetics), Cysteine Endopeptidases (metabolism), Humans, Hydrolysis, Models, Molecular, Molecular Sequence Data, Molecular Structure, Mutation (genetics), Protease Inhibitors (chemical synthesis), Protease Inhibitors (pharmacology), Protein Conformation, Protein Processing, Post-Translational, SARS Virus (enzymology), SARS Virus (genetics), SARS Virus (metabolism), Severe Acute Respiratory Syndrome (genetics), Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization, Substrate Specificity, Viral Proteins (antagonists & inhibitors), Viral Proteins (genetics), Viral Proteins (metabolism).
- MESH :
- chemical , antagonists & inhibitors : Viral Proteins.
- chemical , chemical synthesis : Aldehydes, Protease Inhibitors.
- chemical , genetics : Cysteine Endopeptidases, Viral Proteins.
- chemical , metabolism : Cysteine Endopeptidases, Viral Proteins.
- chemical , pharmacology : Aldehydes, Protease Inhibitors.
- enzymology : SARS Virus.
- genetics : Mutation, SARS Virus, Severe Acute Respiratory Syndrome.
- metabolism : SARS Virus.
- Amino Acid Sequence, Binding Sites, Humans, Hydrolysis, Models, Molecular, Molecular Sequence Data, Molecular Structure, Protein Conformation, Protein Processing, Post-Translational, Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization, Substrate Specificity.
Abstract
The mature SARS 3CL protease is subject to degradation at 188Arg/189Gln. The tetrapeptide sequence is enough for inhibitory activities of peptide-aldehyde inhibitor of the protease.
Url:
DOI: 10.1016/j.bmc.2008.09.057
PubMed: 18845442
PubMed Central: 7126698
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PMC:7126698Le document en format XML
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uniqKey="Konno H" first="Hiroyuki" last="Konno">Hiroyuki Konno</name><affiliation wicri:level="1"><nlm:aff id="aff1">Department of Chemistry, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kita-ku, Kyoto 603-8334, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Chemistry, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kita-ku, Kyoto 603-8334</wicri:regionArea><wicri:noRegion>Kyoto 603-8334</wicri:noRegion></affiliation></author><author><name sortKey="Onozuka, Mari" sort="Onozuka, Mari" uniqKey="Onozuka M" first="Mari" last="Onozuka">Mari Onozuka</name><affiliation wicri:level="1"><nlm:aff id="aff1">Department of Chemistry, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kita-ku, Kyoto 603-8334, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Chemistry, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kita-ku, Kyoto 603-8334</wicri:regionArea><wicri:noRegion>Kyoto 603-8334</wicri:noRegion></affiliation></author><author><name sortKey="Makino, Ayumi" sort="Makino, Ayumi" uniqKey="Makino A" first="Ayumi" last="Makino">Ayumi Makino</name><affiliation wicri:level="1"><nlm:aff id="aff2">Department of Biophysical Chemistry, Kobe Pharmaceutical University, Kobe 658-8558, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Biophysical Chemistry, Kobe Pharmaceutical University, Kobe 658-8558</wicri:regionArea><wicri:noRegion>Kobe 658-8558</wicri:noRegion></affiliation></author><author><name sortKey="Saito, Hiroyuki" sort="Saito, Hiroyuki" uniqKey="Saito H" first="Hiroyuki" last="Saito">Hiroyuki Saito</name><affiliation wicri:level="1"><nlm:aff id="aff2">Department of Biophysical Chemistry, Kobe Pharmaceutical University, Kobe 658-8558, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Biophysical Chemistry, Kobe Pharmaceutical University, Kobe 658-8558</wicri:regionArea><wicri:noRegion>Kobe 658-8558</wicri:noRegion></affiliation></author><author><name sortKey="Nosaka, Kazuto" sort="Nosaka, Kazuto" uniqKey="Nosaka K" first="Kazuto" last="Nosaka">Kazuto Nosaka</name><affiliation wicri:level="1"><nlm:aff id="aff1">Department of Chemistry, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kita-ku, Kyoto 603-8334, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Chemistry, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kita-ku, Kyoto 603-8334</wicri:regionArea><wicri:noRegion>Kyoto 603-8334</wicri:noRegion></affiliation></author></analytic><series><title level="j">Bioorganic & Medicinal Chemistry</title><idno type="ISSN">0968-0896</idno><idno type="eISSN">1464-3391</idno><imprint><date when="2008">2008</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Aldehydes (chemical synthesis)</term><term>Aldehydes (pharmacology)</term><term>Amino Acid Sequence</term><term>Binding Sites</term><term>Cysteine Endopeptidases (genetics)</term><term>Cysteine Endopeptidases (metabolism)</term><term>Humans</term><term>Hydrolysis</term><term>Models, Molecular</term><term>Molecular Sequence Data</term><term>Molecular Structure</term><term>Mutation (genetics)</term><term>Protease Inhibitors (chemical synthesis)</term><term>Protease Inhibitors (pharmacology)</term><term>Protein Conformation</term><term>Protein Processing, Post-Translational</term><term>SARS Virus (enzymology)</term><term>SARS Virus (genetics)</term><term>SARS Virus (metabolism)</term><term>Severe Acute Respiratory Syndrome (genetics)</term><term>Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization</term><term>Substrate Specificity</term><term>Viral Proteins (antagonists & inhibitors)</term><term>Viral Proteins (genetics)</term><term>Viral Proteins (metabolism)</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Aldéhydes (pharmacologie)</term><term>Aldéhydes (synthèse chimique)</term><term>Conformation des protéines</term><term>Cysteine endopeptidases (génétique)</term><term>Cysteine endopeptidases (métabolisme)</term><term>Données de séquences moléculaires</term><term>Humains</term><term>Hydrolyse</term><term>Inhibiteurs de protéases (pharmacologie)</term><term>Inhibiteurs de protéases (synthèse chimique)</term><term>Maturation post-traductionnelle des protéines</term><term>Modèles moléculaires</term><term>Mutation (génétique)</term><term>Protéines virales (antagonistes et inhibiteurs)</term><term>Protéines virales (génétique)</term><term>Protéines virales (métabolisme)</term><term>Sites de fixation</term><term>Spectrométrie de masse MALDI</term><term>Spécificité du substrat</term><term>Structure moléculaire</term><term>Syndrome respiratoire aigu sévère (génétique)</term><term>Séquence d'acides aminés</term><term>Virus du SRAS (enzymologie)</term><term>Virus du SRAS (génétique)</term><term>Virus du SRAS (métabolisme)</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>Aldehydes</term><term>Protease Inhibitors</term></keywords><keywords scheme="MESH" type="chemical" qualifier="genetics" xml:lang="en"><term>Cysteine Endopeptidases</term><term>Viral Proteins</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Cysteine Endopeptidases</term><term>Viral Proteins</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Aldehydes</term><term>Protease Inhibitors</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="genetics" xml:lang="en"><term>Mutation</term><term>SARS Virus</term><term>Severe Acute Respiratory Syndrome</term></keywords><keywords scheme="MESH" qualifier="génétique" xml:lang="fr"><term>Cysteine endopeptidases</term><term>Mutation</term><term>Protéines virales</term><term>Syndrome respiratoire aigu sévère</term><term>Virus du SRAS</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>SARS Virus</term></keywords><keywords scheme="MESH" qualifier="métabolisme" xml:lang="fr"><term>Cysteine endopeptidases</term><term>Protéines virales</term><term>Virus du SRAS</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Aldéhydes</term><term>Inhibiteurs de protéases</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Aldéhydes</term><term>Inhibiteurs de protéases</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Amino Acid Sequence</term><term>Binding Sites</term><term>Humans</term><term>Hydrolysis</term><term>Models, Molecular</term><term>Molecular Sequence Data</term><term>Molecular Structure</term><term>Protein Conformation</term><term>Protein Processing, Post-Translational</term><term>Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization</term><term>Substrate Specificity</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Conformation des protéines</term><term>Données de séquences moléculaires</term><term>Humains</term><term>Hydrolyse</term><term>Maturation post-traductionnelle des protéines</term><term>Modèles moléculaires</term><term>Sites de fixation</term><term>Spectrométrie de masse MALDI</term><term>Spécificité du substrat</term><term>Structure moléculaire</term><term>Séquence d'acides aminés</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en"><title>Graphical abstract</title><p>The mature SARS 3CL protease is subject to degradation at 188Arg/189Gln. The tetrapeptide sequence is enough for inhibitory activities of peptide-aldehyde inhibitor of the protease.</p><fig id="d32e1117" position="anchor"><graphic xlink:href="fx1"></graphic></fig></div></front><back><div1 type="bibliography"><listBibl><biblStruct><analytic><author><name sortKey="Lee, N" uniqKey="Lee N">N. Lee</name></author><author><name sortKey="Hui, D" uniqKey="Hui D">D. Hui</name></author><author><name sortKey="Wu, A" uniqKey="Wu A">A. Wu</name></author><author><name sortKey="Chan, P" uniqKey="Chan P">P. Chan</name></author><author><name sortKey="Cameron, P" uniqKey="Cameron P">P. Cameron</name></author><author><name sortKey="Joynt, F M" uniqKey="Joynt F">F.M. Joynt</name></author><author><name sortKey="Ahuja, A" uniqKey="Ahuja A">A. Ahuja</name></author><author><name sortKey="Yung, M Y" uniqKey="Yung M">M.Y. Yung</name></author><author><name sortKey="Leung, C B" uniqKey="Leung C">C.B. Leung</name></author><author><name sortKey="To, K F" uniqKey="To K">K.F. 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