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RESEARCH PRODUCT
Sortase A Inhibitors: Recent Advances and Future Perspectives
Maria Valeria RaimondiBenedetta MaggioDomenico SchillaciStella CascioferroDemetrio RaffaGiuseppe Daidonesubject
Models MolecularStaphylococcus aureusRhodanineProtein ConformationVirulenceAdamantanemedicine.disease_causeStaphylococcal infectionsSettore BIO/19 - Microbiologia GeneraleBenzoatesBacterial AdhesionSortase A inhibitors review future perspectiveMicrobiologySmall Molecule LibrariesBacterial ProteinsIn vivoDrug DiscoveryNitrilesmedicineAnimalsHumansEnzyme Inhibitorschemistry.chemical_classificationLipid IIbiologyThionesStaphylococcal Infectionsbiology.organism_classificationmedicine.diseaseAminoacyltransferasesSettore CHIM/08 - Chimica FarmaceuticaAmino acidAnti-Bacterial AgentsCysteine EndopeptidasesThiazolesBiochemistrychemistryStaphylococcus aureusSortase AMolecular MedicineBacteriaCarbolinesdescription
Here, we describe the most promising small synthetic organic compounds that act as potent Sortase A inhibitors and cater the potential to be developed as antivirulence drugs. Sortase A is a polypeptide of 206 amino acids, which catalyzes two sequential reactions: (i) thioesterification and (ii) transpeptidation. Sortase A is involved in the process of bacterial adhesion by anchoring LPXTG-containing proteins to lipid II. Sortase A inhibitors do not affect bacterial growth, but they restrain the virulence of pathogenic bacterial strains, thereby preventing infections caused by Staphylococcus aureus or other Gram-positive bacteria. The efficacy of the most promising inhibitors needs to be comprehensively evaluated in in vivo models of infection, in order to select compounds eligible for the treatment of bacterial infections in humans.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2015-12-10 |