Whole Cell Active Inhibitors of Mycobacterial Lipoamide Dehydrogenase Afford Selectivity over the Human Enzyme through Tight Binding Interactions.
inhibitor
lipoamide dehydrogenase
mycobacteria
residence time
slow binding
tight binding
tuberculosis
Journal
ACS infectious diseases
ISSN: 2373-8227
Titre abrégé: ACS Infect Dis
Pays: United States
ID NLM: 101654580
Informations de publication
Date de publication:
12 02 2021
12 02 2021
Historique:
pubmed:
3
2
2021
medline:
24
6
2021
entrez:
2
2
2021
Statut:
ppublish
Résumé
Tuberculosis remains a leading cause of death from a single bacterial infection worldwide. Efforts to develop new treatment options call for expansion into an unexplored target space to expand the drug pipeline and bypass resistance to current antibiotics. Lipoamide dehydrogenase is a metabolic and antioxidant enzyme critical for mycobacterial growth and survival in mice. Sulfonamide analogs were previously identified as potent and selective inhibitors of mycobacterial lipoamide dehydrogenase
Identifiants
pubmed: 33527832
doi: 10.1021/acsinfecdis.0c00788
pmc: PMC7888283
doi:
Substances chimiques
Anti-Bacterial Agents
0
Dihydrolipoamide Dehydrogenase
EC 1.8.1.4
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Langues
eng
Sous-ensembles de citation
IM
Pagination
435-444Subventions
Organisme : NCI NIH HHS
ID : P30 CA008748
Pays : United States
Organisme : NIGMS NIH HHS
ID : R35 GM118080
Pays : United States
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