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The Antibacterial Drug Candidate SBC3 is a Potent Inhibitor of Bacterial Thioredoxin Reductase.
O'Loughlin, Jennie; Napolitano, Silvia; Alkhathami, Fahad; O'Beirne, Cillian; Marhöfer, Daniel; O'Shaughnessy, Megan; Howe, Orla; Tacke, Matthias; Rubini, Marina.
Afiliação
  • O'Loughlin J; School of Chemistry, University College Dublin Belfield, Dublin 4, Ireland.
  • Napolitano S; Department of Molecular Biology and Biophysics, ETH, Otto-Stern-Weg 5, 8093, Zürich, Switzerland.
  • Alkhathami F; School of Chemistry, University College Dublin Belfield, Dublin 4, Ireland.
  • O'Beirne C; School of Chemistry, University College Dublin Belfield, Dublin 4, Ireland.
  • Marhöfer D; School of Chemistry, University College Dublin Belfield, Dublin 4, Ireland.
  • O'Shaughnessy M; School of Biological and Health Sciences, Technical University Dublin, City Campus, Dublin, Ireland.
  • Howe O; School of Biological and Health Sciences, Technical University Dublin, City Campus, Dublin, Ireland.
  • Tacke M; School of Chemistry, University College Dublin Belfield, Dublin 4, Ireland.
  • Rubini M; School of Chemistry, University College Dublin Belfield, Dublin 4, Ireland.
Chembiochem ; 22(6): 1093-1098, 2021 03 16.
Article em En | MEDLINE | ID: mdl-33170522
ABSTRACT
Antibiotic resistance is a growing problem for public health and associated with increasing economic costs and mortality rates. Silver and silver-related compounds have been used for centuries due to their antimicrobial properties. In this work, we show that 1,3-dibenzyl-4,5-diphenyl-imidazol-2-ylidene silver(I) acetate/NHC*-Ag-OAc (SBC3) is a reversible, high affinity inhibitor of E. coli thioredoxin reductase (TrxR; Ki =10.8±1.2 nM). Minimal inhibition concentration (MIC) tests with different E. coli and P. aeruginosa strains demonstrated that SBC3 can efficiently inhibit bacterial cell growth, especially in combination with established antibiotics like gentamicin. Our results show that SBC3 is a promising antibiotic drug candidate targeting bacterial TrxR.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tiorredoxina Dissulfeto Redutase / Proteínas de Escherichia coli / Antibacterianos Idioma: En Ano de publicação: 2021 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tiorredoxina Dissulfeto Redutase / Proteínas de Escherichia coli / Antibacterianos Idioma: En Ano de publicação: 2021 Tipo de documento: Article