Identification of selective inhibitors of Helicobacter pylori IMPDH as a targeted therapy for the infection.
Journal
Scientific reports
ISSN: 2045-2322
Titre abrégé: Sci Rep
Pays: England
ID NLM: 101563288
Informations de publication
Date de publication:
17 01 2019
17 01 2019
Historique:
received:
10
05
2018
accepted:
30
11
2018
entrez:
19
1
2019
pubmed:
19
1
2019
medline:
1
5
2020
Statut:
epublish
Résumé
Helicobacter pylori (H. pylori), the major cause of several gastric disorders has been recognied as a type I carcinogen. By virtue of resistance developed by H. pylori strains, currently used antibiotic based treatments rather demonstrate high failure rates. Hence, there is an emerging need for identification of new targets to treat H. pylori infection. Inosine-5'-monophosphate dehydrogenase (IMPDH) has been studied as a potential target to treat H. pylori infection. Here, a detailed enzyme kinetic study of recombinant expressed H. pylori inosine-5'-monophosphate dehydrogenase (HpIMPDH) is presented. A new in-house synthesized indole-based scaffold is identified as an inhibitor for HpIMPDH. These indole-based compounds showed non-competitive inhibition against IMP and NAD
Identifiants
pubmed: 30655593
doi: 10.1038/s41598-018-37490-x
pii: 10.1038/s41598-018-37490-x
pmc: PMC6336804
doi:
Substances chimiques
Anti-Bacterial Agents
0
Bacterial Proteins
0
Enzyme Inhibitors
0
Indoles
0
Recombinant Proteins
0
indole
8724FJW4M5
IMP Dehydrogenase
EC 1.1.1.205
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
190Références
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