DNA Gyrase as a Target for Quinolones [PDF]
Biomedicines, 2023 Bacterial DNA gyrase is a type II topoisomerase that can introduce negative supercoils to DNA substrates and is a clinically-relevant target for the development of new antibacterials. DNA gyrase is one of the primary targets of quinolones, broad-spectrum
Angela C. Spencer, Siva S. Panda
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Rapid, DNA-induced interface swapping by DNA gyrase [PDF]
eLife, 2022 DNA gyrase, a ubiquitous bacterial enzyme, is a type IIA topoisomerase formed by heterotetramerisation of 2 GyrA subunits and 2 GyrB subunits, to form the active complex.
Thomas RM Germe +5 more
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Design, synthesis, and antibacterial assessment of a new series of ciprofloxacin-based compounds as possible dual DNA gyrase/topoisomerase IV inhibitors [PDF]
Scientific ReportsSimultaneous inhibition of DNA gyrase and topoisomerase IV (Topo IV) is a primary pharmacological strategy to enhance antibacterial efficacy and markedly reduce the emergence of antibiotic resistance.
Lamya H. Al-Wahaibi +4 more
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Insights into antibacterial design: Computational modeling of eugenol derivatives targeting DNA gyrase [PDF]
HeliyonThe rise of antibiotic resistance underscores the urgent need for novel antibacterial agents. DNA gyrase, an essential enzyme involved in bacterial DNA replication, is a promising target for antibacterial therapy.
Heba S. Elsewedy +9 more
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Friend or Foe: Protein Inhibitors of DNA Gyrase [PDF]
BiologyDNA gyrase is essential for the successful replication of circular chromosomes, such as those found in most bacterial species, by relieving topological stressors associated with unwinding the double-stranded genetic material.
Shengfeng Ruan +2 more
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Investigating Escherichia coli Colicin E9 immunity protein interactions with DNA gyrase of Pseudomonas aeruginosa: advanced computational approach for developing novel antimicrobial strategies [PDF]
Scientific ReportsProtein-protein interactions (PPIs) are essential to numerous cellular processes, making a thorough investigation of these interactions crucial for a deeper understanding of molecular mechanisms.
Rihaf Alfaraj +2 more
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In vitro and in silico characterization of Crocatin A from red betel leaves: targeting DNA gyrase B and DNA ligase of Enterococcus faecalis with ADMET-based druglikeness analysis [PDF]
BMC ChemistryDental caries is a disease of tooth tissue that can lead to complications, with Enterococcus faecalis being one of the Gram-positive bacteria that plays a crucial role in the infection process.
Devi Meliani +2 more
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Molecular mechanism of a triazole-containing inhibitor of Mycobacterium tuberculosis DNA gyrase [PDF]
iScienceSummary: Antimicrobial resistance remains a persistent and pressing public health concern. Here, we describe the synthesis of original triazole-containing inhibitors targeting the DNA gyrase, a well-validated drug target for developing new antibiotics ...
Antoine Gedeon +19 more
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Discovery of Benzopyrone-Based Candidates as Potential Antimicrobial and Photochemotherapeutic Agents through Inhibition of DNA Gyrase Enzyme B: Design, Synthesis, In Vitro and In Silico Evaluation [PDF]
PharmaceuticalsBacterial DNA gyrase is considered one of the validated targets for antibacterial drug discovery. Benzopyrones have been reported as promising derivatives that inhibit bacterial DNA gyrase B through competitive binding into the ATP binding site of the B ...
Akram Abd El-Haleem +6 more
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Discovery of new Schiff bases of the disalicylic acid scaffold as DNA gyrase and topoisomerase IV inhibitors endowed with antibacterial properties [PDF]
Frontiers in ChemistryDNA gyrase and topoisomerase IV show great potential as targets for antibacterial medicines. In recent decades, various categories of small molecule inhibitors have been identified; however, none have been effective in the market.
Lamya H. Al-Wahaibi +8 more
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