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Št. zadetkov: 2
Structural aspects of Mycobacterium tuberculosis DNA gyrase targeted by novel bacterial topoisomerase inhibitors
Maja Kokot, Martina Hrast, Lipeng Feng, Lesley A Mitchenall, David M. Lawson, Anthony Maxwell, Tanya Parish, Nikola Minovski, Marko Anderluh
Izvirni znanstveni članek
Oznake: DNA giraza;Mycobacterium tuberculosis;inhibitorji;bakterijske topoizomeraze;NBTIs;DNA gyrase;M. tuberculosis;crystal structure;bifurcated halogen bonds;
In this Letter, we present a small series of novel bacterial topoisomerase inhibitors (NTBIs) that exhibit both potent inhibition of Mycobacterium tuberculosis DNA gyrase and potent antimycobacterial activity. The disclosed crystal structure of M. tuberculosis DNA gyrase in complex with DNA and comp ...
Leto: 2024 Vir: Fakulteta za farmacijo (UL FFA)
Potent DNA gyrase inhibitors bind asymmetrically to their target using symmetrical bifurcated halogen bonds
Anja Kolarič, Thomas Germe, Martina Hrast, Clare E. M. Stevenson, David M. Lawson, Nicolas P. Burton, Judit Vörös, Anthony Maxwell, Nikola Minovski, Marko Anderluh
Izvirni znanstveni članek
Oznake: biokemija;DNK;Escherichia coli;zaviralci;antibacterials;DNA gyrase inhibitors;drug discovery;Staphylococcus aureus;intercalators;novel bacterial topoisomerase inhibitors (NBTIs);symmetrical bifurcated halogen bonds;crystal structure;novel NBTIs mechanism of action;
Novel bacterial type II topoisomerase inhibitors (NBTIs) stabilize single-strand DNA cleavage breaks by DNA gyrase but their exact mechanism of action has remained hypothetical until now. We have designed a small library of NBTIs with an improved DNA gyrase-binding moiety resulting in low nanomolar ...
Leto: 2021 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 2
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