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Evaluation of the published kinase inhibitor set to identify multiple inhibitors of bacterial ATP-dependent mur ligasesHrast, Martina ...The Mur ligases form a series of consecutive enzymes that participate in the intracellular steps of bacterial peptidoglycan biosynthesis. They therefore represent interesting targets for ... antibacterial drug discovery. MurC, D, E and F are all ATP-dependent ligases. Accordingly, with the aim being to find multiple inhibitors of these enzymes, we screened a collection of ATP-competitive kinase inhibitors, on Escherichia coli MurC, D and F, and identified five promising scaffolds that inhibited at least two of these ligases. Compounds 1, 2, 4 and 5 are multiple inhibitors of the whole MurC to MurF cascade that act in the micromolar range (IC50, 32 - 368 microM). NMR-assisted binding studies and steady-state kinetics studies performed on aza-stilbene derivative 1 showed, surprisingly, that it acts as a competitive inhibitor of MurD activity towards D-glutamic acid, and additionally, that its binding to the D-glutamic acid binding site is independent of the enzyme closure promoted by ATP.Source: Journal of enzyme inhibition and medicinal chemistry. - ISSN 1475-6366 (Vol. 34, iss. 1, 2019, str. 1010-1017)Type of material - article, component partPublish date - 2019Language - englishCOBISS.SI-ID - 4715633
Author
Hrast, Martina |
Rožman, Kaja, farmacevtka |
Ogris, Iza |
Škedelj, Veronika, 1983- |
Patin, Delphine |
Sova, Matej, 1979- |
Barreteau, Hélène |
Gobec, Stanislav, 1970- |
Golič Grdadolnik, Simona |
Zega, Anamarija
Topics
Jedrska magnetna resonanca |
Bacterial Mur (MurC-MurF) ligases |
published kinase inhibitor set |
steady-state kinetics measurements |
NMR studies |
antibacterial agents |
Mur ligaze |
NMR študije
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Hrast, Martina | 32036 |
Rožman, Kaja, farmacevtka | 37050 |
Ogris, Iza | 50459 |
Škedelj, Veronika, 1983- | 29903 |
Patin, Delphine | |
Sova, Matej, 1979- | 25490 |
Barreteau, Hélène | |
Gobec, Stanislav, 1970- | 15284 |
Golič Grdadolnik, Simona | 08329 |
Zega, Anamarija | 18633 |
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