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Literature summary for 1.8.1.12 extracted from

  • Etxebeste-Mitxeltorena, M.; Plano, D.; Espuelas, S.; Moreno, E.; Aydillo, C.; Jimenez-Ruiz, A.; Soriano, J.C.G.; Sanmartin, C.
    New amides containing selenium as potent Leishmanicidal agents targeting trypanothione reductase (2020), Antimicrob. Agents Chemother., 65, e00524-20 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
Mepacrine
-
Leishmania infantum
N,N'-(4,4'-diselanediylbis[4,1-phenylene])bisadamantamide
-
Leishmania infantum
N,N'-(4,4'-diselanediylbis[4,1-phenylene])bisfuran-2-carboxamide
-
Leishmania infantum
N,N'-(4,4'-diselanediylbis[4,1-phenylene])bisnaphthamide
-
Leishmania infantum

Organism

Organism UniProt Comment Textmining
Leishmania infantum A4HSF7
-
-

Synonyms

Synonyms Comment Organism
trypanothione reductase
-
Leishmania infantum
TryR
-
Leishmania infantum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00553
-
pH 8.0, 26°C Leishmania infantum N,N'-(4,4'-diselanediylbis[4,1-phenylene])bisnaphthamide
0.014
-
pH 8.0, 26°C Leishmania infantum N,N'-(4,4'-diselanediylbis[4,1-phenylene])bisfuran-2-carboxamide
0.01699
-
pH 8.0, 26°C Leishmania infantum Mepacrine
0.0183
-
pH 8.0, 26°C Leishmania infantum N,N'-(4,4'-diselanediylbis[4,1-phenylene])bisadamantamide

General Information

General Information Comment Organism
drug target the enzyme fulfills most of the more relevant requirements to be an interesting drug target because it is essential for parasite survival, druggable, and absent in the host, where it is replaced by glutathione reductase Leishmania infantum