MaghrebDataLibMedV1, Main, Exploration, bibRecord, 000432

From Dynamic Combinatorial Chemistry to in Vivo Evaluation of Reversible and Irreversible Myeloperoxidase Inhibitors.

Identifieur interne : 000432 ( Main/Exploration ); précédent : 000431; suivant : 000433

From Dynamic Combinatorial Chemistry to in Vivo Evaluation of Reversible and Irreversible Myeloperoxidase Inhibitors.

Auteurs : Jalal Soubhye [Belgique] ; Michel Gelbcke [Belgique] ; Pierre Van Antwerpen [Belgique] ; François Dufrasne [Belgique] ; Mokhtaria Yasmina Boufadi [Algérie] ; Jean Nève [Belgique] ; Paul G. Furtmüller [Autriche] ; Christian Obinger [Autriche] ; Karim Zouaoui Boudjeltia [Belgique] ; Franck Meyer [Belgique]

Source :

ACS medicinal chemistry letters [ 1948-5875 ] ; 2017.

RBID : pubmed:28197313

Abstract

The implementation of dynamic combinatorial libraries allowed the determination of highly active reversible and irreversible inhibitors of myeloperoxidase (MPO) at the nanomolar level. Docking experiments highlighted the interaction between the most active ligands and MPO, and further kinetic studies defined the mode of inhibition of these compounds. Finally, in vivo evaluation showed that one dose of irreversible inhibitors is able to suppress the activity of MPO after inducing inflammation.

DOI: 10.1021/acsmedchemlett.6b00417
PubMed: 28197313
PubMed Central: PMC5304337

Affiliations:

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 Evaluation of Reversible and Irreversible Myeloperoxidase Inhibitors.</title>
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 Evaluation of Reversible and Irreversible Myeloperoxidase Inhibitors.</title>
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<front><div type="abstract" xml:lang="en">The implementation of dynamic combinatorial libraries allowed the determination of highly active reversible and irreversible inhibitors of myeloperoxidase (MPO) at the nanomolar level. Docking experiments highlighted the interaction between the most active ligands and MPO, and further kinetic studies defined the mode of inhibition of these compounds. Finally, <i>in vivo</i>
 evaluation showed that one dose of irreversible inhibitors is able to suppress the activity of MPO after inducing inflammation.</div>
</front>
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<DateRevised><Year>2020</Year>
<Month>09</Month>
<Day>30</Day>
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<Month>Feb</Month>
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<ISOAbbreviation>ACS Med Chem Lett</ISOAbbreviation>
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<ArticleTitle>From Dynamic Combinatorial Chemistry to <i>in Vivo</i>
 Evaluation of Reversible and Irreversible Myeloperoxidase Inhibitors.</ArticleTitle>
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<ELocationID EIdType="doi" ValidYN="Y">10.1021/acsmedchemlett.6b00417</ELocationID>
<Abstract><AbstractText>The implementation of dynamic combinatorial libraries allowed the determination of highly active reversible and irreversible inhibitors of myeloperoxidase (MPO) at the nanomolar level. Docking experiments highlighted the interaction between the most active ligands and MPO, and further kinetic studies defined the mode of inhibition of these compounds. Finally, <i>in vivo</i>
 evaluation showed that one dose of irreversible inhibitors is able to suppress the activity of MPO after inducing inflammation.</AbstractText>
</Abstract>
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<ForeName>Jalal</ForeName>
<Initials>J</Initials>
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<Author ValidYN="Y"><LastName>Furtmüller</LastName>
<ForeName>Paul G</ForeName>
<Initials>PG</Initials>
<AffiliationInfo><Affiliation>Department of Chemistry, BOKU-University of Natural Resources and Life Sciences , 1190 Vienna, Austria.</Affiliation>
</AffiliationInfo>
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<Author ValidYN="Y"><LastName>Obinger</LastName>
<ForeName>Christian</ForeName>
<Initials>C</Initials>
<AffiliationInfo><Affiliation>Department of Chemistry, BOKU-University of Natural Resources and Life Sciences , 1190 Vienna, Austria.</Affiliation>
</AffiliationInfo>
</Author>
<Author ValidYN="Y"><LastName>Zouaoui Boudjeltia</LastName>
<ForeName>Karim</ForeName>
<Initials>K</Initials>
<AffiliationInfo><Affiliation>Laboratory of Experimental Medicine (ULB 222 unit), Université Libre de Bruxelles, Chu de Charleroi , 6110 Belgium.</Affiliation>
</AffiliationInfo>
</Author>
<Author ValidYN="Y"><LastName>Meyer</LastName>
<ForeName>Franck</ForeName>
<Initials>F</Initials>
<AffiliationInfo><Affiliation>Laboratory of Biopolymers and Supramolecular Nanomaterials, Faculty of Pharmacy, Université Libre de Bruxelles (ULB) , Boulevard du Triomphe, 1050 Bruxelles, Belgium.</Affiliation>
</AffiliationInfo>
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<Language>eng</Language>
<PublicationTypeList><PublicationType UI="D016428">Journal Article</PublicationType>
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<ArticleDate DateType="Electronic"><Year>2016</Year>
<Month>12</Month>
<Day>02</Day>
</ArticleDate>
</Article>
<MedlineJournalInfo><Country>United States</Country>
<MedlineTA>ACS Med Chem Lett</MedlineTA>
<NlmUniqueID>101521073</NlmUniqueID>
<ISSNLinking>1948-5875</ISSNLinking>
</MedlineJournalInfo>
<KeywordList Owner="NOTNLM"><Keyword MajorTopicYN="N">Myeloperoxidase</Keyword>
<Keyword MajorTopicYN="N">dynamic combinatorial chemistry</Keyword>
<Keyword MajorTopicYN="N">kinetic study</Keyword>
<Keyword MajorTopicYN="N">molecular docking</Keyword>
<Keyword MajorTopicYN="N">reversible and irreversible inhibitors</Keyword>
</KeywordList>
<CoiStatement>The authors declare no competing financial interest.</CoiStatement>
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<PubmedData><History><PubMedPubDate PubStatus="received"><Year>2016</Year>
<Month>10</Month>
<Day>20</Day>
</PubMedPubDate>
<PubMedPubDate PubStatus="accepted"><Year>2016</Year>
<Month>12</Month>
<Day>02</Day>
</PubMedPubDate>
<PubMedPubDate PubStatus="entrez"><Year>2017</Year>
<Month>2</Month>
<Day>16</Day>
<Hour>6</Hour>
<Minute>0</Minute>
</PubMedPubDate>
<PubMedPubDate PubStatus="pubmed"><Year>2017</Year>
<Month>2</Month>
<Day>16</Day>
<Hour>6</Hour>
<Minute>0</Minute>
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<PubMedPubDate PubStatus="medline"><Year>2017</Year>
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<Day>16</Day>
<Hour>6</Hour>
<Minute>1</Minute>
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<ArticleId IdType="doi">10.1021/acsmedchemlett.6b00417</ArticleId>
<ArticleId IdType="pmc">PMC5304337</ArticleId>
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</pubmed>
<affiliations><list><country><li>Algérie</li>
<li>Autriche</li>
<li>Belgique</li>
</country>
<region><li>Région de Bruxelles-Capitale</li>
<li>Vienne (Autriche)</li>
</region>
<settlement><li>Bruxelles</li>
<li>Vienne (Autriche)</li>
</settlement>
<orgName><li>Université libre de Bruxelles</li>
</orgName>
</list>
<tree><country name="Belgique"><region name="Région de Bruxelles-Capitale"><name sortKey="Soubhye, Jalal" sort="Soubhye, Jalal" uniqKey="Soubhye J" first="Jalal" last="Soubhye">Jalal Soubhye</name>
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<name sortKey="Dufrasne, Francois" sort="Dufrasne, Francois" uniqKey="Dufrasne F" first="François" last="Dufrasne">François Dufrasne</name>
<name sortKey="Gelbcke, Michel" sort="Gelbcke, Michel" uniqKey="Gelbcke M" first="Michel" last="Gelbcke">Michel Gelbcke</name>
<name sortKey="Meyer, Franck" sort="Meyer, Franck" uniqKey="Meyer F" first="Franck" last="Meyer">Franck Meyer</name>
<name sortKey="Neve, Jean" sort="Neve, Jean" uniqKey="Neve J" first="Jean" last="Nève">Jean Nève</name>
<name sortKey="Van Antwerpen, Pierre" sort="Van Antwerpen, Pierre" uniqKey="Van Antwerpen P" first="Pierre" last="Van Antwerpen">Pierre Van Antwerpen</name>
<name sortKey="Zouaoui Boudjeltia, Karim" sort="Zouaoui Boudjeltia, Karim" uniqKey="Zouaoui Boudjeltia K" first="Karim" last="Zouaoui Boudjeltia">Karim Zouaoui Boudjeltia</name>
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<country name="Autriche"><region name="Vienne (Autriche)"><name sortKey="Furtmuller, Paul G" sort="Furtmuller, Paul G" uniqKey="Furtmuller P" first="Paul G" last="Furtmüller">Paul G. Furtmüller</name>
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From Dynamic Combinatorial Chemistry to in Vivo Evaluation of Reversible and Irreversible Myeloperoxidase Inhibitors.

From Dynamic Combinatorial Chemistry to in Vivo Evaluation of Reversible and Irreversible Myeloperoxidase Inhibitors.

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