-
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.Vir: Journal of enzyme inhibition and medicinal chemistry. - ISSN 1475-6366 (Vol. 34, iss. 1, 2019, str. 1010-1017)Vrsta gradiva - članek, sestavni delLeto - 2019Jezik - angleškiCOBISS.SI-ID - 4715633
Avtor
Hrast, Martina |
Rožman, Kaja, farmacevtka |
Ogris, Iza |
Škedelj, Veronika, farmacevtka |
Patin, Delphine |
Sova, Matej, 1979- |
Barreteau, Hélène |
Gobec, Stanislav, 1970- |
Golič Grdadolnik, Simona |
Zega, Anamarija
Teme
Jedrska magnetna resonanca |
Bacterial Mur (MurC-MurF) ligases |
published kinase inhibitor set |
steady-state kinetics measurements |
NMR studies |
antibacterial agents |
Mur ligaze |
NMR študije
![loading ... loading ...](themes/default/img/ajax-loading.gif)
vir: Journal of enzyme inhibition and medicinal chemistry. - ISSN 1475-6366 (Vol. 34, iss. 1, 2019, str. 1010-1017)
![loading ... loading ...](themes/default/img/ajax-loading.gif)
![loading ... loading ...](themes/default/img/ajax-loading.gif)
![loading ... loading ...](themes/default/img/ajax-loading.gif)
Vnos na polico
Trajna povezava
- URL:
Faktor vpliva
Dostop do baze podatkov JCR je dovoljen samo uporabnikom iz Slovenije. Vaš trenutni IP-naslov ni na seznamu dovoljenih za dostop, zato je potrebna avtentikacija z ustreznim računom AAI.
Leto | Faktor vpliva | Izdaja | Kategorija | Razvrstitev | ||||
---|---|---|---|---|---|---|---|---|
JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Baze podatkov, v katerih je revija indeksirana
Ime baze podatkov | Področje | Leto |
---|
Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
---|---|
Hrast, Martina | 32036 |
Rožman, Kaja, farmacevtka | 37050 |
Ogris, Iza | 50459 |
Škedelj, Veronika, farmacevtka | 29903 |
Patin, Delphine | ![]() |
Sova, Matej, 1979- | 25490 |
Barreteau, Hélène | ![]() |
Gobec, Stanislav, 1970- | 15284 |
Golič Grdadolnik, Simona | 08329 |
Zega, Anamarija | 18633 |
Izberite prevzemno mesto:
Prevzem gradiva po pošti
Obvestilo
Gesla v Splošnem geslovniku COBISS
Izbira mesta prevzema
Mesto prevzema | Status gradiva | Rezervacija |
---|
Prosimo, počakajte trenutek.