Recent Advances in Inhibitors of Bacterial Fatty Acid Synthesis Type II (FASII) System Enzymes as Potential Antibacterial Agents
Identifieur interne : 001178 ( Main/Exploration ); précédent : 001177; suivant : 001179Recent Advances in Inhibitors of Bacterial Fatty Acid Synthesis Type II (FASII) System Enzymes as Potential Antibacterial Agents
Auteurs : Yi Wang [République populaire de Chine] ; Shutao Ma [République populaire de Chine]Source :
- ChemMedChem [ 1860-7179 ] ; 2013-10.
English descriptors
- Teeft :
- Acta crystallogr, Active site, Active sites, Aeruginosa, Agents chemother, Aliphatic chain, Analogue, Antibacterial, Antibacterial activities, Antibacterial activity, Antibacterial agents, Antimicrob, Aureus, Aureus fabh, Aureus fabi, Aureus fabio, Binding mode, Binding model, Biochem, Biochemistry, Biol, Biological activities, Bioorg, Biosynthesis, Carbonyl, Carbonyl group, Catalytic mechanism, Catalytic triad, Chem, Chemmedchem, Chemmedchem minireviews, Chemother, Clinical trials, Cofactor, Coli, Coli fabh, Coli fabi, Coli fabis, Coli kasiii, Compound, Covalent adduct, Cronan, Derivative, Drug discovery, Elongation pathway, Enzyme, Faba, Fabb, Fabf, Fabg, Fabh, Fabh inhibitors, Fabi, Fabio, Fabis, Fabk, Fabl, Fabv, Fabz, Falciparum, Falciparum fabi, Falciparum strains, Falk, Fasii, Fasii inhibitors, Fasii system, Fatty acid biosynthesis, Free enzyme, Further optimization, Gmbh, Good activity, Heath, Herath, Hydrogen bond, Hydrogen bonds, Hydrophobic interaction, Hydroxy, Iida, Inha, Inhibitor, Janson, Jayasuriya, Kaplan, Kgaa, Kitagawa, Lett, Microbiol, Minireviews, Moiety, Mrsa, Nicotinamide ring, Ondeyka, Optimization, Oxygen atom, Pathogen, Pathway, Perozzo, Phenol, Platencin, Pneumoniae, Potent activities, Potent activity, Pylori fabz, Pylorus, Recent advances, Reductase, Several inhibitors, Significant activity, Singh, Sohn, Subtilis, System enzymes, Takahata, Tetrahedron lett, Tonge, Triclosan, Tuberculosis fabh, Tuberculosis inha, Uncompetitive inhibitor, Verlag, Verlag gmbh, Vivo efficacy, Wang, Weinheim, Weinheim chemmedchem, Wide range, Zhang, Zheng.
Abstract
Bacterial infections are a constant and serious threat to human health. With the increase of multidrug resistance of clinically pathogenic bacteria, common antibiotic therapies have been less effective. Fatty acid synthesis type II (FASII) system enzymes are essential for bacterial membrane lipid biosynthesis and represent increasingly promising targets for the discovery of antibacterial agents with new mechanisms of action. This review highlights recent advances in inhibitors of bacterial FASII as potential antibacterial agents, paying special attention to the activities, mechanisms, and structure–activity relationships of those inhibitors that mainly target β‐ketoacyl‐ACP synthase, β‐ketoacyl‐ACP reductase, β‐hydroxyacyl‐ACP dehydratase, and enoyl‐ACP reductase. Although inhibitors with low nanomolar and selective activity against various bacterial FASII have entered clinical trials, further research is needed to expand upon both available and yet unknown scaffolds to identify new FASII inhibitors that may have antibacterial potential, particularly against resistant bacterial strains.
Fast to fight infection: Bacterial infections remain a major global health concern. The fatty acid synthesis type II (FASII) pathway is a potential target used for the discovery and development of antibacterial agents with novel mechanisms of action. This review highlights recent advances in FASII inhibitors, with particular focus on their activities, structure–activity relationships, and mechanisms.
Url:
DOI: 10.1002/cmdc.201300209
Affiliations:
Links toward previous steps (curation, corpus...)
- to stream Istex, to step Corpus: 002556
- to stream Istex, to step Curation: 002556
- to stream Istex, to step Checkpoint: 000230
- to stream Main, to step Merge: 001179
- to stream Main, to step Curation: 001178
Le document en format XML
<record><TEI wicri:istexFullTextTei="biblStruct"><teiHeader><fileDesc><titleStmt><title xml:lang="en">Recent Advances in Inhibitors of Bacterial Fatty Acid Synthesis Type II (FASII) System Enzymes as Potential Antibacterial Agents</title><author><name sortKey="Wang, Yi" sort="Wang, Yi" uniqKey="Wang Y" first="Yi" last="Wang">Yi Wang</name></author><author><name sortKey="Ma, Shutao" sort="Ma, Shutao" uniqKey="Ma S" first="Shutao" last="Ma">Shutao Ma</name></author></titleStmt><publicationStmt><idno type="wicri:source">ISTEX</idno><idno type="RBID">ISTEX:8E91C10BD8078DDB06F2EE353EE2366E6E25E79C</idno><date when="2013" year="2013">2013</date><idno type="doi">10.1002/cmdc.201300209</idno><idno type="url">https://api.istex.fr/ark:/67375/WNG-WB105N6P-1/fulltext.pdf</idno><idno type="wicri:Area/Istex/Corpus">002556</idno><idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Corpus" wicri:corpus="ISTEX">002556</idno><idno type="wicri:Area/Istex/Curation">002556</idno><idno type="wicri:Area/Istex/Checkpoint">000230</idno><idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Checkpoint">000230</idno><idno type="wicri:doubleKey">1860-7179:2013:Wang Y:recent:advances:in</idno><idno type="wicri:Area/Main/Merge">001179</idno><idno type="wicri:Area/Main/Curation">001178</idno><idno type="wicri:Area/Main/Exploration">001178</idno></publicationStmt><sourceDesc><biblStruct><analytic><title level="a" type="main">Recent Advances in Inhibitors of Bacterial Fatty Acid Synthesis Type II (FASII) System Enzymes as Potential Antibacterial Agents</title><author><name sortKey="Wang, Yi" sort="Wang, Yi" uniqKey="Wang Y" first="Yi" last="Wang">Yi Wang</name><affiliation wicri:level="1"><country xml:lang="fr" wicri:curation="lc">République populaire de Chine</country><wicri:regionArea>Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road</wicri:regionArea><wicri:noRegion>44 West Culture Road</wicri:noRegion></affiliation></author><author><name sortKey="Ma, Shutao" sort="Ma, Shutao" uniqKey="Ma S" first="Shutao" last="Ma">Shutao Ma</name><affiliation wicri:level="1"><country xml:lang="fr" wicri:curation="lc">République populaire de Chine</country><wicri:regionArea>Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road</wicri:regionArea><wicri:noRegion>44 West Culture Road</wicri:noRegion></affiliation><affiliation wicri:level="1"><country wicri:rule="url">République populaire de Chine</country></affiliation><affiliation wicri:level="1"><country xml:lang="fr" wicri:curation="lc">République populaire de Chine</country><wicri:regionArea>Correspondence address: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road</wicri:regionArea><wicri:noRegion>44 West Culture Road</wicri:noRegion></affiliation></author></analytic><monogr></monogr><series><title level="j" type="main">ChemMedChem</title><title level="j" type="alt">CHEMMEDCHEM</title><idno type="ISSN">1860-7179</idno><idno type="eISSN">1860-7187</idno><imprint><biblScope unit="vol">8</biblScope><biblScope unit="issue">10</biblScope><biblScope unit="page" from="1589">1589</biblScope><biblScope unit="page" to="1608">1608</biblScope><biblScope unit="page-count">20</biblScope><publisher>WILEY‐VCH Verlag</publisher><pubPlace>Weinheim</pubPlace><date type="published" when="2013-10">2013-10</date></imprint><idno type="ISSN">1860-7179</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">1860-7179</idno></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="Teeft" xml:lang="en"><term>Acta crystallogr</term><term>Active site</term><term>Active sites</term><term>Aeruginosa</term><term>Agents chemother</term><term>Aliphatic chain</term><term>Analogue</term><term>Antibacterial</term><term>Antibacterial activities</term><term>Antibacterial activity</term><term>Antibacterial agents</term><term>Antimicrob</term><term>Aureus</term><term>Aureus fabh</term><term>Aureus fabi</term><term>Aureus fabio</term><term>Binding mode</term><term>Binding model</term><term>Biochem</term><term>Biochemistry</term><term>Biol</term><term>Biological activities</term><term>Bioorg</term><term>Biosynthesis</term><term>Carbonyl</term><term>Carbonyl group</term><term>Catalytic mechanism</term><term>Catalytic triad</term><term>Chem</term><term>Chemmedchem</term><term>Chemmedchem minireviews</term><term>Chemother</term><term>Clinical trials</term><term>Cofactor</term><term>Coli</term><term>Coli fabh</term><term>Coli fabi</term><term>Coli fabis</term><term>Coli kasiii</term><term>Compound</term><term>Covalent adduct</term><term>Cronan</term><term>Derivative</term><term>Drug discovery</term><term>Elongation pathway</term><term>Enzyme</term><term>Faba</term><term>Fabb</term><term>Fabf</term><term>Fabg</term><term>Fabh</term><term>Fabh inhibitors</term><term>Fabi</term><term>Fabio</term><term>Fabis</term><term>Fabk</term><term>Fabl</term><term>Fabv</term><term>Fabz</term><term>Falciparum</term><term>Falciparum fabi</term><term>Falciparum strains</term><term>Falk</term><term>Fasii</term><term>Fasii inhibitors</term><term>Fasii system</term><term>Fatty acid biosynthesis</term><term>Free enzyme</term><term>Further optimization</term><term>Gmbh</term><term>Good activity</term><term>Heath</term><term>Herath</term><term>Hydrogen bond</term><term>Hydrogen bonds</term><term>Hydrophobic interaction</term><term>Hydroxy</term><term>Iida</term><term>Inha</term><term>Inhibitor</term><term>Janson</term><term>Jayasuriya</term><term>Kaplan</term><term>Kgaa</term><term>Kitagawa</term><term>Lett</term><term>Microbiol</term><term>Minireviews</term><term>Moiety</term><term>Mrsa</term><term>Nicotinamide ring</term><term>Ondeyka</term><term>Optimization</term><term>Oxygen atom</term><term>Pathogen</term><term>Pathway</term><term>Perozzo</term><term>Phenol</term><term>Platencin</term><term>Pneumoniae</term><term>Potent activities</term><term>Potent activity</term><term>Pylori fabz</term><term>Pylorus</term><term>Recent advances</term><term>Reductase</term><term>Several inhibitors</term><term>Significant activity</term><term>Singh</term><term>Sohn</term><term>Subtilis</term><term>System enzymes</term><term>Takahata</term><term>Tetrahedron lett</term><term>Tonge</term><term>Triclosan</term><term>Tuberculosis fabh</term><term>Tuberculosis inha</term><term>Uncompetitive inhibitor</term><term>Verlag</term><term>Verlag gmbh</term><term>Vivo efficacy</term><term>Wang</term><term>Weinheim</term><term>Weinheim chemmedchem</term><term>Wide range</term><term>Zhang</term><term>Zheng</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Bacterial infections are a constant and serious threat to human health. With the increase of multidrug resistance of clinically pathogenic bacteria, common antibiotic therapies have been less effective. Fatty acid synthesis type II (FASII) system enzymes are essential for bacterial membrane lipid biosynthesis and represent increasingly promising targets for the discovery of antibacterial agents with new mechanisms of action. This review highlights recent advances in inhibitors of bacterial FASII as potential antibacterial agents, paying special attention to the activities, mechanisms, and structure–activity relationships of those inhibitors that mainly target β‐ketoacyl‐ACP synthase, β‐ketoacyl‐ACP reductase, β‐hydroxyacyl‐ACP dehydratase, and enoyl‐ACP reductase. Although inhibitors with low nanomolar and selective activity against various bacterial FASII have entered clinical trials, further research is needed to expand upon both available and yet unknown scaffolds to identify new FASII inhibitors that may have antibacterial potential, particularly against resistant bacterial strains.</div><div type="abstract" xml:lang="en">Fast to fight infection: Bacterial infections remain a major global health concern. The fatty acid synthesis type II (FASII) pathway is a potential target used for the discovery and development of antibacterial agents with novel mechanisms of action. This review highlights recent advances in FASII inhibitors, with particular focus on their activities, structure–activity relationships, and mechanisms.</div></front></TEI><affiliations><list><country><li>République populaire de Chine</li></country></list><tree><country name="République populaire de Chine"><noRegion><name sortKey="Wang, Yi" sort="Wang, Yi" uniqKey="Wang Y" first="Yi" last="Wang">Yi Wang</name></noRegion><name sortKey="Ma, Shutao" sort="Ma, Shutao" uniqKey="Ma S" first="Shutao" last="Ma">Shutao Ma</name><name sortKey="Ma, Shutao" sort="Ma, Shutao" uniqKey="Ma S" first="Shutao" last="Ma">Shutao Ma</name><name sortKey="Ma, Shutao" sort="Ma, Shutao" uniqKey="Ma S" first="Shutao" last="Ma">Shutao Ma</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Sante/explor/ChloroquineV1/Data/Main/Exploration
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 001178 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 001178 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien
|wiki= Sante
|area= ChloroquineV1
|flux= Main
|étape= Exploration
|type= RBID
|clé= ISTEX:8E91C10BD8078DDB06F2EE353EE2366E6E25E79C
|texte= Recent Advances in Inhibitors of Bacterial Fatty Acid Synthesis Type II (FASII) System Enzymes as Potential Antibacterial Agents
}}
| This area was generated with Dilib version V0.6.33. |  |