Characterization of Lead Compounds Targeting the Selenoprotein Thioredoxin Glutathione Reductase for Treatment of Schistosomiasis.
Animals
Drug Discovery
Enzyme Inhibitors
/ pharmacology
High-Throughput Screening Assays
Inhibitory Concentration 50
Mice
Multienzyme Complexes
/ antagonists & inhibitors
NADH, NADPH Oxidoreductases
/ antagonists & inhibitors
NADP
/ metabolism
Oxidation-Reduction
/ drug effects
Schistosoma mansoni
/ drug effects
Schistosomiasis
/ drug therapy
Schistosomicides
/ pharmacology
drug development
helminth
high throughput screen
mechanism of inhibition
neglected disease
redox biology
Journal
ACS infectious diseases
ISSN: 2373-8227
Titre abrégé: ACS Infect Dis
Pays: United States
ID NLM: 101654580
Informations de publication
Date de publication:
13 03 2020
13 03 2020
Historique:
pubmed:
16
1
2020
medline:
28
1
2021
entrez:
16
1
2020
Statut:
ppublish
Résumé
Schistosomiasis is a widespread human parasitic disease currently affecting over 200 million people. Chemotherapy for schistosomiasis relies exclusively on praziquantel. Although significant advances have been made in recent years to reduce the incidence and intensity of schistosome infections, these gains will be at risk should drug-resistant parasites evolve. Thioredoxin glutathione reductase (TGR) is a selenoprotein of the parasite essential for the survival of schistosomes in the mammalian host. Several high-throughput screening campaigns have identified inhibitors of
Identifiants
pubmed: 31939288
doi: 10.1021/acsinfecdis.9b00354
pmc: PMC7072008
mid: NIHMS1068542
doi:
Substances chimiques
Enzyme Inhibitors
0
Multienzyme Complexes
0
Schistosomicides
0
NADP
53-59-8
NADH, NADPH Oxidoreductases
EC 1.6.-
thioredoxin glutathione reductase
EC 1.6.4.-
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
393-405Subventions
Organisme : NIAID NIH HHS
ID : HHSN272201700014C
Pays : United States
Organisme : NIAID NIH HHS
ID : R33 AI127635
Pays : United States
Organisme : NIAID NIH HHS
ID : HHSN272201300014I
Pays : United States
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