Novel chloroacetamido compound CWR-J02 is an anti-inflammatory glutaredoxin-1 inhibitor.
Identifieur interne : 000336 ( Main/Exploration ); précédent : 000335; suivant : 000337Novel chloroacetamido compound CWR-J02 is an anti-inflammatory glutaredoxin-1 inhibitor.
Auteurs : Olga Gorelenkova Miller [États-Unis] ; Kyle S. Cole [États-Unis] ; Corey C. Emerson [États-Unis] ; Dharmaraja Allimuthu [États-Unis] ; Marcin Golczak [États-Unis] ; Phoebe L. Stewart [États-Unis] ; Eranthie Weerapana [États-Unis] ; Drew J. Adams [États-Unis] ; John J. Mieyal [États-Unis]Source :
- PloS one [ 1932-6203 ] ; 2017.
Descripteurs français
- KwdFr :
- Acides phtaliques (pharmacologie), Acides phtaliques (synthèse chimique), Acétanilides (pharmacologie), Acétanilides (synthèse chimique), Animaux (MeSH), Anti-inflammatoires (pharmacologie), Anti-inflammatoires (synthèse chimique), Biotine (composition chimique), Chimie click (MeSH), Cinétique (MeSH), Expression des gènes (MeSH), Glutarédoxines (antagonistes et inhibiteurs), Glutarédoxines (composition chimique), Glutarédoxines (génétique), Glutarédoxines (métabolisme), Liaison aux protéines (MeSH), Lignée cellulaire (MeSH), Lipopolysaccharides (antagonistes et inhibiteurs), Lipopolysaccharides (pharmacologie), Microglie (cytologie), Microglie (effets des médicaments et des substances chimiques), Microglie (métabolisme), Motifs et domaines d'intéraction protéique (MeSH), Protéines recombinantes (composition chimique), Protéines recombinantes (génétique), Protéines recombinantes (métabolisme), Simulation de dynamique moléculaire (MeSH), Sites de fixation (MeSH), Souris (MeSH), Streptavidine (composition chimique), Structure en brin bêta (MeSH), Structure en hélice alpha (MeSH), Séquence d'acides aminés (MeSH), Tests de criblage à haut débit (MeSH), Thermodynamique (MeSH).
- MESH :
- antagonistes et inhibiteurs : Glutarédoxines, Lipopolysaccharides.
- composition chimique : Biotine, Glutarédoxines, Protéines recombinantes, Streptavidine.
- cytologie : Microglie.
- effets des médicaments et des substances chimiques : Microglie.
- génétique : Glutarédoxines, Protéines recombinantes.
- métabolisme : Glutarédoxines, Microglie, Protéines recombinantes.
- pharmacologie : Acides phtaliques, Acétanilides, Anti-inflammatoires, Lipopolysaccharides.
- synthèse chimique : Acides phtaliques, Acétanilides, Anti-inflammatoires.
- Animaux, Chimie click, Cinétique, Expression des gènes, Liaison aux protéines, Lignée cellulaire, Motifs et domaines d'intéraction protéique, Simulation de dynamique moléculaire, Sites de fixation, Souris, Structure en brin bêta, Structure en hélice alpha, Séquence d'acides aminés, Tests de criblage à haut débit, Thermodynamique.
English descriptors
- KwdEn :
- Acetanilides (chemical synthesis), Acetanilides (pharmacology), Amino Acid Sequence (MeSH), Animals (MeSH), Anti-Inflammatory Agents (chemical synthesis), Anti-Inflammatory Agents (pharmacology), Binding Sites (MeSH), Biotin (chemistry), Cell Line (MeSH), Click Chemistry (MeSH), Gene Expression (MeSH), Glutaredoxins (antagonists & inhibitors), Glutaredoxins (chemistry), Glutaredoxins (genetics), Glutaredoxins (metabolism), High-Throughput Screening Assays (MeSH), Kinetics (MeSH), Lipopolysaccharides (antagonists & inhibitors), Lipopolysaccharides (pharmacology), Mice (MeSH), Microglia (cytology), Microglia (drug effects), Microglia (metabolism), Molecular Dynamics Simulation (MeSH), Phthalic Acids (chemical synthesis), Phthalic Acids (pharmacology), Protein Binding (MeSH), Protein Conformation, alpha-Helical (MeSH), Protein Conformation, beta-Strand (MeSH), Protein Interaction Domains and Motifs (MeSH), Recombinant Proteins (chemistry), Recombinant Proteins (genetics), Recombinant Proteins (metabolism), Streptavidin (chemistry), Thermodynamics (MeSH).
- MESH :
- chemical , antagonists & inhibitors : Glutaredoxins, Lipopolysaccharides.
- chemical , chemical synthesis : Acetanilides, Anti-Inflammatory Agents, Phthalic Acids.
- chemical , chemistry : Biotin, Glutaredoxins, Recombinant Proteins, Streptavidin.
- chemical , genetics : Glutaredoxins, Recombinant Proteins.
- chemical , metabolism : Glutaredoxins, Recombinant Proteins.
- chemical , pharmacology : Acetanilides, Anti-Inflammatory Agents, Lipopolysaccharides, Phthalic Acids.
- cytology : Microglia.
- drug effects : Microglia.
- metabolism : Microglia.
- Amino Acid Sequence, Animals, Binding Sites, Cell Line, Click Chemistry, Gene Expression, High-Throughput Screening Assays, Kinetics, Mice, Molecular Dynamics Simulation, Protein Binding, Protein Conformation, alpha-Helical, Protein Conformation, beta-Strand, Protein Interaction Domains and Motifs, Thermodynamics.
Abstract
Glutaredoxin (Grx1) is a ubiquitously expressed thiol-disulfide oxidoreductase that specifically catalyzes reduction of S-glutathionylated substrates. Grx1 is known to be a key regulator of pro-inflammatory signaling, and Grx1 silencing inhibits inflammation in inflammatory disease models. Therefore, we anticipate that inhibition of Grx1 could be an anti-inflammatory therapeutic strategy. We used a rapid screening approach to test 504 novel electrophilic compounds for inhibition of Grx1, which has a highly reactive active-site cysteine residue (pKa 3.5). From this chemical library a chloroacetamido compound, CWR-J02, was identified as a potential lead compound to be characterized. CWR-J02 inhibited isolated Grx1 with an IC50 value of 32 μM in the presence of 1 mM glutathione. Mass spectrometric analysis documented preferential adduction of CWR-J02 to the active site Cys-22 of Grx1, and molecular dynamics simulation identified a potential non-covalent binding site. Treatment of the BV2 microglial cell line with CWR-J02 led to inhibition of intracellular Grx1 activity with an IC50 value (37 μM). CWR-J02 treatment decreased lipopolysaccharide-induced inflammatory gene transcription in the microglial cells in a parallel concentration-dependent manner, documenting the anti-inflammatory potential of CWR-J02. Exploiting the alkyne moiety of CWR-J02, we used click chemistry to link biotin azide to CWR-J02-adducted proteins, isolating them with streptavidin beads. Tandem mass spectrometric analysis identified many CWR-J02-reactive proteins, including Grx1 and several mediators of inflammatory activation. Taken together, these data identify CWR-J02 as an intracellularly effective Grx1 inhibitor that may elicit its anti-inflammatory action in a synergistic manner by also disabling other pro-inflammatory mediators. The CWR-J02 molecule provides a starting point for developing more selective Grx1 inhibitors and anti-inflammatory agents for therapeutic development.
DOI: 10.1371/journal.pone.0187991
PubMed: 29155853
PubMed Central: PMC5695812
Affiliations:
Links toward previous steps (curation, corpus...)
Le document en format XML
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<author><name sortKey="Stewart, Phoebe L" sort="Stewart, Phoebe L" uniqKey="Stewart P" first="Phoebe L" last="Stewart">Phoebe L. Stewart</name>
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<author><name sortKey="Weerapana, Eranthie" sort="Weerapana, Eranthie" uniqKey="Weerapana E" first="Eranthie" last="Weerapana">Eranthie Weerapana</name>
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<author><name sortKey="Mieyal, John J" sort="Mieyal, John J" uniqKey="Mieyal J" first="John J" last="Mieyal">John J. Mieyal</name>
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<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Acetanilides (chemical synthesis)</term>
<term>Acetanilides (pharmacology)</term>
<term>Amino Acid Sequence (MeSH)</term>
<term>Animals (MeSH)</term>
<term>Anti-Inflammatory Agents (chemical synthesis)</term>
<term>Anti-Inflammatory Agents (pharmacology)</term>
<term>Binding Sites (MeSH)</term>
<term>Biotin (chemistry)</term>
<term>Cell Line (MeSH)</term>
<term>Click Chemistry (MeSH)</term>
<term>Gene Expression (MeSH)</term>
<term>Glutaredoxins (antagonists & inhibitors)</term>
<term>Glutaredoxins (chemistry)</term>
<term>Glutaredoxins (genetics)</term>
<term>Glutaredoxins (metabolism)</term>
<term>High-Throughput Screening Assays (MeSH)</term>
<term>Kinetics (MeSH)</term>
<term>Lipopolysaccharides (antagonists & inhibitors)</term>
<term>Lipopolysaccharides (pharmacology)</term>
<term>Mice (MeSH)</term>
<term>Microglia (cytology)</term>
<term>Microglia (drug effects)</term>
<term>Microglia (metabolism)</term>
<term>Molecular Dynamics Simulation (MeSH)</term>
<term>Phthalic Acids (chemical synthesis)</term>
<term>Phthalic Acids (pharmacology)</term>
<term>Protein Binding (MeSH)</term>
<term>Protein Conformation, alpha-Helical (MeSH)</term>
<term>Protein Conformation, beta-Strand (MeSH)</term>
<term>Protein Interaction Domains and Motifs (MeSH)</term>
<term>Recombinant Proteins (chemistry)</term>
<term>Recombinant Proteins (genetics)</term>
<term>Recombinant Proteins (metabolism)</term>
<term>Streptavidin (chemistry)</term>
<term>Thermodynamics (MeSH)</term>
</keywords>
<keywords scheme="KwdFr" xml:lang="fr"><term>Acides phtaliques (pharmacologie)</term>
<term>Acides phtaliques (synthèse chimique)</term>
<term>Acétanilides (pharmacologie)</term>
<term>Acétanilides (synthèse chimique)</term>
<term>Animaux (MeSH)</term>
<term>Anti-inflammatoires (pharmacologie)</term>
<term>Anti-inflammatoires (synthèse chimique)</term>
<term>Biotine (composition chimique)</term>
<term>Chimie click (MeSH)</term>
<term>Cinétique (MeSH)</term>
<term>Expression des gènes (MeSH)</term>
<term>Glutarédoxines (antagonistes et inhibiteurs)</term>
<term>Glutarédoxines (composition chimique)</term>
<term>Glutarédoxines (génétique)</term>
<term>Glutarédoxines (métabolisme)</term>
<term>Liaison aux protéines (MeSH)</term>
<term>Lignée cellulaire (MeSH)</term>
<term>Lipopolysaccharides (antagonistes et inhibiteurs)</term>
<term>Lipopolysaccharides (pharmacologie)</term>
<term>Microglie (cytologie)</term>
<term>Microglie (effets des médicaments et des substances chimiques)</term>
<term>Microglie (métabolisme)</term>
<term>Motifs et domaines d'intéraction protéique (MeSH)</term>
<term>Protéines recombinantes (composition chimique)</term>
<term>Protéines recombinantes (génétique)</term>
<term>Protéines recombinantes (métabolisme)</term>
<term>Simulation de dynamique moléculaire (MeSH)</term>
<term>Sites de fixation (MeSH)</term>
<term>Souris (MeSH)</term>
<term>Streptavidine (composition chimique)</term>
<term>Structure en brin bêta (MeSH)</term>
<term>Structure en hélice alpha (MeSH)</term>
<term>Séquence d'acides aminés (MeSH)</term>
<term>Tests de criblage à haut débit (MeSH)</term>
<term>Thermodynamique (MeSH)</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>Glutaredoxins</term>
<term>Lipopolysaccharides</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Acetanilides</term>
<term>Anti-Inflammatory Agents</term>
<term>Phthalic Acids</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Biotin</term>
<term>Glutaredoxins</term>
<term>Recombinant Proteins</term>
<term>Streptavidin</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="genetics" xml:lang="en"><term>Glutaredoxins</term>
<term>Recombinant Proteins</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Glutaredoxins</term>
<term>Recombinant Proteins</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Acetanilides</term>
<term>Anti-Inflammatory Agents</term>
<term>Lipopolysaccharides</term>
<term>Phthalic Acids</term>
</keywords>
<keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr"><term>Glutarédoxines</term>
<term>Lipopolysaccharides</term>
</keywords>
<keywords scheme="MESH" qualifier="composition chimique" xml:lang="fr"><term>Biotine</term>
<term>Glutarédoxines</term>
<term>Protéines recombinantes</term>
<term>Streptavidine</term>
</keywords>
<keywords scheme="MESH" qualifier="cytologie" xml:lang="fr"><term>Microglie</term>
</keywords>
<keywords scheme="MESH" qualifier="cytology" xml:lang="en"><term>Microglia</term>
</keywords>
<keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Microglia</term>
</keywords>
<keywords scheme="MESH" qualifier="effets des médicaments et des substances chimiques" xml:lang="fr"><term>Microglie</term>
</keywords>
<keywords scheme="MESH" qualifier="génétique" xml:lang="fr"><term>Glutarédoxines</term>
<term>Protéines recombinantes</term>
</keywords>
<keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Microglia</term>
</keywords>
<keywords scheme="MESH" qualifier="métabolisme" xml:lang="fr"><term>Glutarédoxines</term>
<term>Microglie</term>
<term>Protéines recombinantes</term>
</keywords>
<keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Acides phtaliques</term>
<term>Acétanilides</term>
<term>Anti-inflammatoires</term>
<term>Lipopolysaccharides</term>
</keywords>
<keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Acides phtaliques</term>
<term>Acétanilides</term>
<term>Anti-inflammatoires</term>
</keywords>
<keywords scheme="MESH" xml:lang="en"><term>Amino Acid Sequence</term>
<term>Animals</term>
<term>Binding Sites</term>
<term>Cell Line</term>
<term>Click Chemistry</term>
<term>Gene Expression</term>
<term>High-Throughput Screening Assays</term>
<term>Kinetics</term>
<term>Mice</term>
<term>Molecular Dynamics Simulation</term>
<term>Protein Binding</term>
<term>Protein Conformation, alpha-Helical</term>
<term>Protein Conformation, beta-Strand</term>
<term>Protein Interaction Domains and Motifs</term>
<term>Thermodynamics</term>
</keywords>
<keywords scheme="MESH" xml:lang="fr"><term>Animaux</term>
<term>Chimie click</term>
<term>Cinétique</term>
<term>Expression des gènes</term>
<term>Liaison aux protéines</term>
<term>Lignée cellulaire</term>
<term>Motifs et domaines d'intéraction protéique</term>
<term>Simulation de dynamique moléculaire</term>
<term>Sites de fixation</term>
<term>Souris</term>
<term>Structure en brin bêta</term>
<term>Structure en hélice alpha</term>
<term>Séquence d'acides aminés</term>
<term>Tests de criblage à haut débit</term>
<term>Thermodynamique</term>
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<front><div type="abstract" xml:lang="en">Glutaredoxin (Grx1) is a ubiquitously expressed thiol-disulfide oxidoreductase that specifically catalyzes reduction of S-glutathionylated substrates. Grx1 is known to be a key regulator of pro-inflammatory signaling, and Grx1 silencing inhibits inflammation in inflammatory disease models. Therefore, we anticipate that inhibition of Grx1 could be an anti-inflammatory therapeutic strategy. We used a rapid screening approach to test 504 novel electrophilic compounds for inhibition of Grx1, which has a highly reactive active-site cysteine residue (pKa 3.5). From this chemical library a chloroacetamido compound, CWR-J02, was identified as a potential lead compound to be characterized. CWR-J02 inhibited isolated Grx1 with an IC50 value of 32 μM in the presence of 1 mM glutathione. Mass spectrometric analysis documented preferential adduction of CWR-J02 to the active site Cys-22 of Grx1, and molecular dynamics simulation identified a potential non-covalent binding site. Treatment of the BV2 microglial cell line with CWR-J02 led to inhibition of intracellular Grx1 activity with an IC50 value (37 μM). CWR-J02 treatment decreased lipopolysaccharide-induced inflammatory gene transcription in the microglial cells in a parallel concentration-dependent manner, documenting the anti-inflammatory potential of CWR-J02. Exploiting the alkyne moiety of CWR-J02, we used click chemistry to link biotin azide to CWR-J02-adducted proteins, isolating them with streptavidin beads. Tandem mass spectrometric analysis identified many CWR-J02-reactive proteins, including Grx1 and several mediators of inflammatory activation. Taken together, these data identify CWR-J02 as an intracellularly effective Grx1 inhibitor that may elicit its anti-inflammatory action in a synergistic manner by also disabling other pro-inflammatory mediators. The CWR-J02 molecule provides a starting point for developing more selective Grx1 inhibitors and anti-inflammatory agents for therapeutic development.</div>
</front>
</TEI>
<pubmed><MedlineCitation Status="MEDLINE" Owner="NLM"><PMID Version="1">29155853</PMID>
<DateCompleted><Year>2017</Year>
<Month>12</Month>
<Day>19</Day>
</DateCompleted>
<DateRevised><Year>2018</Year>
<Month>11</Month>
<Day>13</Day>
</DateRevised>
<Article PubModel="Electronic-eCollection"><Journal><ISSN IssnType="Electronic">1932-6203</ISSN>
<JournalIssue CitedMedium="Internet"><Volume>12</Volume>
<Issue>11</Issue>
<PubDate><Year>2017</Year>
</PubDate>
</JournalIssue>
<Title>PloS one</Title>
<ISOAbbreviation>PLoS One</ISOAbbreviation>
</Journal>
<ArticleTitle>Novel chloroacetamido compound CWR-J02 is an anti-inflammatory glutaredoxin-1 inhibitor.</ArticleTitle>
<Pagination><MedlinePgn>e0187991</MedlinePgn>
</Pagination>
<ELocationID EIdType="doi" ValidYN="Y">10.1371/journal.pone.0187991</ELocationID>
<Abstract><AbstractText>Glutaredoxin (Grx1) is a ubiquitously expressed thiol-disulfide oxidoreductase that specifically catalyzes reduction of S-glutathionylated substrates. Grx1 is known to be a key regulator of pro-inflammatory signaling, and Grx1 silencing inhibits inflammation in inflammatory disease models. Therefore, we anticipate that inhibition of Grx1 could be an anti-inflammatory therapeutic strategy. We used a rapid screening approach to test 504 novel electrophilic compounds for inhibition of Grx1, which has a highly reactive active-site cysteine residue (pKa 3.5). From this chemical library a chloroacetamido compound, CWR-J02, was identified as a potential lead compound to be characterized. CWR-J02 inhibited isolated Grx1 with an IC50 value of 32 μM in the presence of 1 mM glutathione. Mass spectrometric analysis documented preferential adduction of CWR-J02 to the active site Cys-22 of Grx1, and molecular dynamics simulation identified a potential non-covalent binding site. Treatment of the BV2 microglial cell line with CWR-J02 led to inhibition of intracellular Grx1 activity with an IC50 value (37 μM). CWR-J02 treatment decreased lipopolysaccharide-induced inflammatory gene transcription in the microglial cells in a parallel concentration-dependent manner, documenting the anti-inflammatory potential of CWR-J02. Exploiting the alkyne moiety of CWR-J02, we used click chemistry to link biotin azide to CWR-J02-adducted proteins, isolating them with streptavidin beads. Tandem mass spectrometric analysis identified many CWR-J02-reactive proteins, including Grx1 and several mediators of inflammatory activation. Taken together, these data identify CWR-J02 as an intracellularly effective Grx1 inhibitor that may elicit its anti-inflammatory action in a synergistic manner by also disabling other pro-inflammatory mediators. The CWR-J02 molecule provides a starting point for developing more selective Grx1 inhibitors and anti-inflammatory agents for therapeutic development.</AbstractText>
</Abstract>
<AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Gorelenkova Miller</LastName>
<ForeName>Olga</ForeName>
<Initials>O</Initials>
<AffiliationInfo><Affiliation>Department of Pharmacology, Case Western Reserve University, Cleveland, Ohio, United States of America.</Affiliation>
</AffiliationInfo>
</Author>
<Author ValidYN="Y"><LastName>Cole</LastName>
<ForeName>Kyle S</ForeName>
<Initials>KS</Initials>
<AffiliationInfo><Affiliation>Department of Chemistry, Boston College, Chestnut Hill, Massachusetts, United States of America.</Affiliation>
</AffiliationInfo>
</Author>
<Author ValidYN="Y"><LastName>Emerson</LastName>
<ForeName>Corey C</ForeName>
<Initials>CC</Initials>
<AffiliationInfo><Affiliation>Department of Pharmacology, Case Western Reserve University, Cleveland, Ohio, United States of America.</Affiliation>
</AffiliationInfo>
</Author>
<Author ValidYN="Y"><LastName>Allimuthu</LastName>
<ForeName>Dharmaraja</ForeName>
<Initials>D</Initials>
<AffiliationInfo><Affiliation>Department of Genetics, Case Western Reserve University, Cleveland, Ohio, United States of America.</Affiliation>
</AffiliationInfo>
</Author>
<Author ValidYN="Y"><LastName>Golczak</LastName>
<ForeName>Marcin</ForeName>
<Initials>M</Initials>
<AffiliationInfo><Affiliation>Department of Pharmacology, Case Western Reserve University, Cleveland, Ohio, United States of America.</Affiliation>
</AffiliationInfo>
<AffiliationInfo><Affiliation>Cleveland Center for Membrane and Structural Biology, Case Western Reserve University, Cleveland, Ohio, United States of America.</Affiliation>
</AffiliationInfo>
</Author>
<Author ValidYN="Y"><LastName>Stewart</LastName>
<ForeName>Phoebe L</ForeName>
<Initials>PL</Initials>
<AffiliationInfo><Affiliation>Department of Pharmacology, Case Western Reserve University, Cleveland, Ohio, United States of America.</Affiliation>
</AffiliationInfo>
<AffiliationInfo><Affiliation>Cleveland Center for Membrane and Structural Biology, Case Western Reserve University, Cleveland, Ohio, United States of America.</Affiliation>
</AffiliationInfo>
</Author>
<Author ValidYN="Y"><LastName>Weerapana</LastName>
<ForeName>Eranthie</ForeName>
<Initials>E</Initials>
<AffiliationInfo><Affiliation>Department of Chemistry, Boston College, Chestnut Hill, Massachusetts, United States of America.</Affiliation>
</AffiliationInfo>
</Author>
<Author ValidYN="Y"><LastName>Adams</LastName>
<ForeName>Drew J</ForeName>
<Initials>DJ</Initials>
<AffiliationInfo><Affiliation>Department of Genetics, Case Western Reserve University, Cleveland, Ohio, United States of America.</Affiliation>
</AffiliationInfo>
</Author>
<Author ValidYN="Y"><LastName>Mieyal</LastName>
<ForeName>John J</ForeName>
<Initials>JJ</Initials>
<Identifier Source="ORCID">http://orcid.org/0000-0002-8957-6334</Identifier>
<AffiliationInfo><Affiliation>Department of Pharmacology, Case Western Reserve University, Cleveland, Ohio, United States of America.</Affiliation>
</AffiliationInfo>
<AffiliationInfo><Affiliation>Cleveland Center for Membrane and Structural Biology, Case Western Reserve University, Cleveland, Ohio, United States of America.</Affiliation>
</AffiliationInfo>
</Author>
</AuthorList>
<Language>eng</Language>
<GrantList CompleteYN="Y"><Grant><GrantID>S10 RR031537</GrantID>
<Acronym>RR</Acronym>
<Agency>NCRR NIH HHS</Agency>
<Country>United States</Country>
</Grant>
<Grant><GrantID>R21 NS085503</GrantID>
<Acronym>NS</Acronym>
<Agency>NINDS NIH HHS</Agency>
<Country>United States</Country>
</Grant>
<Grant><GrantID>I01 BX000290</GrantID>
<Acronym>BX</Acronym>
<Agency>BLRD VA</Agency>
<Country>United States</Country>
</Grant>
<Grant><GrantID>R01 EY023948</GrantID>
<Acronym>EY</Acronym>
<Agency>NEI NIH HHS</Agency>
<Country>United States</Country>
</Grant>
<Grant><GrantID>T32 GM008803</GrantID>
<Acronym>GM</Acronym>
<Agency>NIGMS NIH HHS</Agency>
<Country>United States</Country>
</Grant>
<Grant><GrantID>R01 GM118431</GrantID>
<Acronym>GM</Acronym>
<Agency>NIGMS NIH HHS</Agency>
<Country>United States</Country>
</Grant>
</GrantList>
<PublicationTypeList><PublicationType UI="D016428">Journal Article</PublicationType>
</PublicationTypeList>
<ArticleDate DateType="Electronic"><Year>2017</Year>
<Month>11</Month>
<Day>20</Day>
</ArticleDate>
</Article>
<MedlineJournalInfo><Country>United States</Country>
<MedlineTA>PLoS One</MedlineTA>
<NlmUniqueID>101285081</NlmUniqueID>
<ISSNLinking>1932-6203</ISSNLinking>
</MedlineJournalInfo>
<ChemicalList><Chemical><RegistryNumber>0</RegistryNumber>
<NameOfSubstance UI="D000083">Acetanilides</NameOfSubstance>
</Chemical>
<Chemical><RegistryNumber>0</RegistryNumber>
<NameOfSubstance UI="D000893">Anti-Inflammatory Agents</NameOfSubstance>
</Chemical>
<Chemical><RegistryNumber>0</RegistryNumber>
<NameOfSubstance UI="C000625552">CWR-J02</NameOfSubstance>
</Chemical>
<Chemical><RegistryNumber>0</RegistryNumber>
<NameOfSubstance UI="C516006">Glrx protein, mouse</NameOfSubstance>
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<Chemical><RegistryNumber>0</RegistryNumber>
<NameOfSubstance UI="D054477">Glutaredoxins</NameOfSubstance>
</Chemical>
<Chemical><RegistryNumber>0</RegistryNumber>
<NameOfSubstance UI="D008070">Lipopolysaccharides</NameOfSubstance>
</Chemical>
<Chemical><RegistryNumber>0</RegistryNumber>
<NameOfSubstance UI="D010795">Phthalic Acids</NameOfSubstance>
</Chemical>
<Chemical><RegistryNumber>0</RegistryNumber>
<NameOfSubstance UI="D011994">Recombinant Proteins</NameOfSubstance>
</Chemical>
<Chemical><RegistryNumber>6SO6U10H04</RegistryNumber>
<NameOfSubstance UI="D001710">Biotin</NameOfSubstance>
</Chemical>
<Chemical><RegistryNumber>9013-20-1</RegistryNumber>
<NameOfSubstance UI="D019809">Streptavidin</NameOfSubstance>
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</ChemicalList>
<CitationSubset>IM</CitationSubset>
<MeshHeadingList><MeshHeading><DescriptorName UI="D000083" MajorTopicYN="N">Acetanilides</DescriptorName>
<QualifierName UI="Q000138" MajorTopicYN="N">chemical synthesis</QualifierName>
<QualifierName UI="Q000494" MajorTopicYN="Y">pharmacology</QualifierName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D000595" MajorTopicYN="N">Amino Acid Sequence</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D000818" MajorTopicYN="N">Animals</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D000893" MajorTopicYN="N">Anti-Inflammatory Agents</DescriptorName>
<QualifierName UI="Q000138" MajorTopicYN="N">chemical synthesis</QualifierName>
<QualifierName UI="Q000494" MajorTopicYN="Y">pharmacology</QualifierName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D001665" MajorTopicYN="N">Binding Sites</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D001710" MajorTopicYN="N">Biotin</DescriptorName>
<QualifierName UI="Q000737" MajorTopicYN="N">chemistry</QualifierName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D002460" MajorTopicYN="N">Cell Line</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D057930" MajorTopicYN="N">Click Chemistry</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D015870" MajorTopicYN="N">Gene Expression</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D054477" MajorTopicYN="N">Glutaredoxins</DescriptorName>
<QualifierName UI="Q000037" MajorTopicYN="Y">antagonists & inhibitors</QualifierName>
<QualifierName UI="Q000737" MajorTopicYN="N">chemistry</QualifierName>
<QualifierName UI="Q000235" MajorTopicYN="N">genetics</QualifierName>
<QualifierName UI="Q000378" MajorTopicYN="N">metabolism</QualifierName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D057166" MajorTopicYN="N">High-Throughput Screening Assays</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D007700" MajorTopicYN="N">Kinetics</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D008070" MajorTopicYN="N">Lipopolysaccharides</DescriptorName>
<QualifierName UI="Q000037" MajorTopicYN="N">antagonists & inhibitors</QualifierName>
<QualifierName UI="Q000494" MajorTopicYN="N">pharmacology</QualifierName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D051379" MajorTopicYN="N">Mice</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D017628" MajorTopicYN="N">Microglia</DescriptorName>
<QualifierName UI="Q000166" MajorTopicYN="N">cytology</QualifierName>
<QualifierName UI="Q000187" MajorTopicYN="Y">drug effects</QualifierName>
<QualifierName UI="Q000378" MajorTopicYN="N">metabolism</QualifierName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D056004" MajorTopicYN="N">Molecular Dynamics Simulation</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D010795" MajorTopicYN="N">Phthalic Acids</DescriptorName>
<QualifierName UI="Q000138" MajorTopicYN="N">chemical synthesis</QualifierName>
<QualifierName UI="Q000494" MajorTopicYN="Y">pharmacology</QualifierName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D011485" MajorTopicYN="N">Protein Binding</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D000072756" MajorTopicYN="N">Protein Conformation, alpha-Helical</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D000072757" MajorTopicYN="N">Protein Conformation, beta-Strand</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D054730" MajorTopicYN="N">Protein Interaction Domains and Motifs</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D011994" MajorTopicYN="N">Recombinant Proteins</DescriptorName>
<QualifierName UI="Q000737" MajorTopicYN="N">chemistry</QualifierName>
<QualifierName UI="Q000235" MajorTopicYN="N">genetics</QualifierName>
<QualifierName UI="Q000378" MajorTopicYN="N">metabolism</QualifierName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D019809" MajorTopicYN="N">Streptavidin</DescriptorName>
<QualifierName UI="Q000737" MajorTopicYN="N">chemistry</QualifierName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D013816" MajorTopicYN="N">Thermodynamics</DescriptorName>
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<PubmedData><History><PubMedPubDate PubStatus="received"><Year>2017</Year>
<Month>07</Month>
<Day>06</Day>
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<PubMedPubDate PubStatus="accepted"><Year>2017</Year>
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