Exploitation of a Novel Allosteric Binding Region in DNA Gyrase and its Implications for Antibacterial Drug Discovery

Orritt, Kyle; Maxwell, Anthony; Fishwick, Colin W. G.; McPhillie, Martin J.

doi:10.4155/fmc-2021-0266

Cited by 5 publications

(3 citation statements)

References 15 publications

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“…Our approach demonstrates that a combination of traditional medicinal chemistry and in silico molecular modelling can identify new scaffolds for this target and may lay the foundations to identify future novel gyrase and topo IV antibacterial agents. 26 …”

Section: Discussionmentioning

confidence: 99%

De novo design of type II topoisomerase inhibitors as potential antimicrobial agents targeting a novel binding region

et al. 2022

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Section: Discussionmentioning

confidence: 99%

De novo design of type II topoisomerase inhibitors as potential antimicrobial agents targeting a novel binding region

et al. 2022

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“…H-bond interactions between benzothiazole and naphthalene with dihydroorotase (at sites LEU222 or ASN44) led to inhibition of E. coli dihydroorotase enzyme, and this may contribute to the antimicrobial effect of these compounds (Morsy et al 2020). Topo isomerase II is an attractive target for the development of new antibacterial agents as it plays a key role in stabilizing the topological state of the DNA (Khan et al 2018;Orritt et al 2021). We found that, the compounds with higher concentrations presented in the ethanolic extract of A. graecorum interact with the DNA-Topo ll in a position and orientation similar to the original inhibitor ligand (07N).…”

Section: Discussionmentioning

confidence: 99%

Potential synergistic effect of Alhagi graecorum ethanolic extract with two conventional food preservatives against some foodborne pathogens

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Marrez

Ali

et al. 2022

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The present study aim to screen the antibacterial activity and synergistic interaction of A. graecorum Boiss. ethanolic extract with two food preservatives against five strains of foodborne bacteria. Disk diffusion and minimum inhibitory concentration were used for antibacterial assay, checkerboard assay and time-kill curve were used for the combination studies. HPLC analysis and molecular docking study were performed to corroborate the in vitro results. The ethanolic extract showed antibacterial activity against all tested bacterial strains with inhibition zones from 7.5 to 9.3 mm and MIC values ranged between 1.2 and 1.8 mg ml− 1. The combination of the ethanolic extract with Na-benzoate or Na-propionate resulted in synergistic and additive interactions against the tested bacteria with fractional inhibitory concentration index (FICI) ranges 0.31–0.63 and no antagonism was shown. Time-kill curve assay showed that the synergistic and additive combinations have inhibitory effects on the tested strains. The ethanolic extract combination with Na-benzoate or Na-propionate can be used for development new sources of food preservatives. Testing new different natural plant extracts with food preservatives will help develop new antibacterial agents.

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“…H-bond interactions between benzothiazole and naphthalene with dihydroorotase (at sites LEU222 or ASN44) led to inhibition of E. coli dihydroorotase enzyme, and this may contribute to the antimicrobial effect of these compounds (Morsy et al 2020 ). Topoisomerase II is an attractive target for the development of new anti-bacterial agents as it plays a key role in stabilizing the topological state of the DNA (Khan et al 2018 ; Orritt et al 2021 ). We found that, the compounds with higher concentrations presented in the ethanolic extract of A. graecorum interact with the DNA Topo ll in a position and orientation similar to the original inhibitor ligand (07N).…”

Section: Discussionmentioning

confidence: 99%

Potential synergistic effect of Alhagi graecorum ethanolic extract with two conventional food preservatives against some foodborne pathogens

et al. 2022

View full text Add to dashboard Cite

The present study aims to screen the anti-bacterial activity and synergistic interaction of A. graecorum Boiss. ethanolic extract with two food preservatives against five strains of foodborne bacteria. Disk diffusion and minimum inhibitory concentration were used for anti-bacterial assay, checkerboard assay and time-kill curve were used for the combination studies. HPLC analysis and molecular docking study were performed to corroborate the in vitro results. The ethanolic extract showed anti-bacterial activity against all tested bacterial strains with inhibition zones from 7.5 to 9.3 mm and MIC values ranged between 1.2 and 1.8 mg mL−1. The combination of the ethanolic extract with Na-benzoate or Na-propionate resulted in synergistic and additive interactions against the tested bacteria with fractional inhibitory concentration index (FICI) ranges 0.31–0.63 and no antagonism was shown. Time-kill curve assay showed that the synergistic and additive combinations have inhibitory effects on the tested strains. The ethanolic extract combination with Na-benzoate or Na-propionate can be used for development new sources of food preservatives. Testing new different natural plant extracts with food preservatives will help develop new anti-bacterial agents.

show abstract

Exploitation of a Novel Allosteric Binding Region in DNA Gyrase and its Implications for Antibacterial Drug Discovery

Cited by 5 publications

References 15 publications

De novo design of type II topoisomerase inhibitors as potential antimicrobial agents targeting a novel binding region

De novo design of type II topoisomerase inhibitors as potential antimicrobial agents targeting a novel binding region

Potential synergistic effect of Alhagi graecorum ethanolic extract with two conventional food preservatives against some foodborne pathogens

Potential synergistic effect of Alhagi graecorum ethanolic extract with two conventional food preservatives against some foodborne pathogens

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