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Literature summary for 1.8.1.12 extracted from

  • Lenz, M.; Krauth-Siegel, R.L.; Schmidt, T.J.
    Natural sesquiterpene lactones of the 4,15-iso-atriplicolide type are inhibitors of trypanothione reductase (2019), Molecules, 24, 3737 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
4,15-iso-atriplicolide isobutyrate 0.1 mM, 15 min, 62% inhibition. The enzyme is inhibited by 4,15-iso-atriplicolide esters in its reduced dithiol state Trypanosoma brucei rhodesiense
4,15-iso-atriplicolide isobutyrate 0.1 mM, 15 min, 80% inhibition Trypanosoma cruzi
4,15-iso-atriplicolide methacrylate 0.1 mM, 15 min, 68% inhibition. The enzyme is inhibited by 4,15-iso-atriplicolide esters in its reduced dithiol state Trypanosoma brucei rhodesiense
4,15-iso-atriplicolide methacrylate 0.1 mM, 15 min, 41% inhibition Trypanosoma cruzi
4,15-iso-atriplicolide tiglate 0.1 mM, 15 min, 87% inhibition. The enzyme is inhibited by 4,15-iso-atriplicolide esters in its reduced dithiol state Trypanosoma brucei rhodesiense
4,15-iso-atriplicolide tiglate 0.1 mM, 15 min, 89% inhibition Trypanosoma cruzi

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
trypanothione disulfide + NADPH + H+ Trypanosoma brucei rhodesiense
-
trypanothione + NADP+
-
?
trypanothione disulfide + NADPH + H+ Trypanosoma cruzi
-
trypanothione + NADP+
-
?

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei rhodesiense
-
-
-
Trypanosoma cruzi P28593
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Trypanosoma brucei rhodesiense
-
Trypanosoma cruzi

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
trypanothione disulfide + NADPH + H+
-
Trypanosoma brucei rhodesiense trypanothione + NADP+
-
?
trypanothione disulfide + NADPH + H+
-
Trypanosoma cruzi trypanothione + NADP+
-
?

Synonyms

Synonyms Comment Organism
TbTR
-
Trypanosoma brucei rhodesiense
TcTR
-
Trypanosoma cruzi
TR
-
Trypanosoma brucei rhodesiense
TR
-
Trypanosoma cruzi
trypanothione reductase
-
Trypanosoma brucei rhodesiense
trypanothione reductase
-
Trypanosoma cruzi

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.128
-
4,15-iso-atriplicolide tiglate pH 7.5, 25°C Trypanosoma brucei rhodesiense