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Št. zadetkov: 2
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)
Exploring the 5-substituted 2-aminobenzothiazole-based DNA gyrase B inhibitors active against ESKAPE pathogens
Maša Sterle, Martina Durcik, Clare E. M. Stevenson, Sara R. Henderson, Petra Eva Szili, Marton Czikkely, David M. Lawson, Danijel Kikelj, Nace Zidar, Lucija Peterlin-Mašič, Janez Ilaš, Tihomir Tomašić, Andrej Emanuel Cotman, Anamarija Zega
Izvirni znanstveni članek
Oznake: inhibitorji;organske kisline;proteini;bacteria;genetics;inhibitors;organic acids;peptides;proteins;
We present a new series of 2-aminobenzothiazole-based DNA gyrase B inhibitors with promising activity against ESKAPE bacterial pathogens. Based on the binding information extracted from the cocrystal structure of DNA gyrase B inhibitor A, in complex with Escherichia coli GyrB24, we expanded the chem ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 2
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