Bacterial persisters are rare phenotypic variants that are suspected to be culprits of recurrent infections. Fluoroquinolones (FQs) are a class of antibiotics that facilitate bacterial killing by stabilizing bacterial type II topoisomerases when they are in a complex with cleaved DNA. In Escherichia coli, DNA gyrase is the primary FQ target, and previous work has demonstrated that persisters are not spared from FQ-induced DNA damage. Since DNA gyrase cleavage sites (GCSs) largely govern the sites of DNA damage from FQ treatment, we hypothesized that GCS characteristics (e.g. number, strength, location) may influence persistence. To test this hypothesis, we measured genome-wide GCS distributions after treatment with a panel of FQs in stationary-phase cultures. We found drug-specific effects on the GCS distribution and discovered a strong negative correlation between the genomic cleavage strength and FQ persister levels. Further experiments and analyses suggested that persistence was unlikely to be governed by cleavage to individual sites, but rather survival was a function of the genomic GCS distribution. Together, these findings demonstrate FQ-specific differences in GCS distribution that correlate with persister levels and suggest that FQs that better stabilize DNA gyrase in cleaved complexes with DNA will lead to lower levels of persistence.
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http://dx.doi.org/10.1093/nar/gkac1223 | DOI Listing |
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Tecnologico de Monterrey, Escuela de Ingeniería y Ciencias, Av. Gral. Ramón Corona No 2514, Colonia Nuevo México, Zapopan 45121, Mexico.
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January 2025
Department of Microbiology, Virology and Immunology, I. Horbachevsky Ternopil State Medical University, 46001 Ternopil, Ukraine.
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January 2025
Department of Chemical Biology, Helmholtz Centre for Infection Research, Inhoffenstraße 7, 38124, Braunschweig, Germany.
The rise of antimicrobial resistance represents a significant global health threat, driven by the diminishing efficacy of existing antibiotics, a lack of novel antibacterials entering the market, and an over- or misuse of existing antibiotics, which accelerates the evolution of resistant bacterial strains. This review focuses on innovative therapies by highlighting 19 novel antibacterials in clinical development as of June 2024. These selected compounds are characterized by new chemical scaffolds, novel molecular targets, and/or unique mechanisms of action, which render their potential to break antimicrobial resistance particularly high.
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January 2025
Department of Medicinal Chemistry, Institute of Medical Sciences, Banaras Hindu University Varanasi UP-221005 India
The antibacterial efficacy of some newly developed bis- and C3-carboxylic moieties of fluoroquinolone-linked triazole conjugates was studied. Twenty compounds from two different series of triazoles were synthesized using click chemistry and evaluated for their antibacterial activity against a Gram-positive strain, (ATCC29212), and its clinical isolate and a Gram-negative bacterial strain, (ATCC25922), and its clinical isolate. Among the compounds, 7, 9a, 9d, 9i, 10(a-d), and 10i showed excellent activity with MIC values of up to 6.
View Article and Find Full Text PDFNPJ Antimicrob Resist
November 2024
Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI) and Saarland University Department of Pharmacy, Campus Building E8.1, 66123, Saarbrücken, Germany.
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