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Literature summary for 1.8.1.12 extracted from

  • Henderson, G.B.; Ulrich, P.; Fairlamb, A.H.; Rosenberg, I.; Pereira, M.; Sela, M.; Cerami, A.
    Subversive substrates for the enzyme trypanothione disulfide reductase: alternative approach to chemotherapy of Chagas disease (1988), Proc. Natl. Acad. Sci. USA, 85, 5374-5378.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
additional information activity is dependent on a redox-active cysteine at the active centre Crithidia fasciculata
additional information activity is dependent on a redox-active cysteine at the active centre Trypanosoma cruzi

Application

Application Comment Organism
medicine inhibition of the enzyme by naphthoquinone and nitrofuran derivatives abolish the cell penetration by the parasite trypomasstigotes, alternate approach to chemotherapy of trypanosomiasis and leishmaniasis, Chagas' disease Crithidia fasciculata
medicine inhibition of the enzyme by naphthoquinone and nitrofuran derivatives abolish the cell penetration by the parasite trypomasstigotes, alternate approach to chemotherapy of trypanosomiasis and leishmaniasis, Chagas' disease Trypanosoma cruzi

Inhibitors

Inhibitors Comment Organism Structure
nifurtimox
-
Trypanosoma cruzi

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Crithidia fasciculata
-
insect-parasitic trypanosomatid
-
Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information naphthoquinones and nitrofuran derivatives are reduced, inhibition of the enzyme Crithidia fasciculata ?
-
?
additional information naphthoquinones and nitrofuran derivatives are reduced, inhibition of the enzyme Trypanosoma cruzi ?
-
?
trypanothione disulfide + NADPH
-
Crithidia fasciculata trypanothione + NADP+
-
?
trypanothione disulfide + NADPH
-
Crithidia fasciculata trypanothione + NADP+
-
r
trypanothione disulfide + NADPH
-
Trypanosoma cruzi trypanothione + NADP+
-
?
trypanothione disulfide + NADPH
-
Trypanosoma cruzi trypanothione + NADP+
-
r

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
27
-
assay at Crithidia fasciculata
27
-
assay at Trypanosoma cruzi

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.8
-
assay at Crithidia fasciculata
7.8
-
assay at Trypanosoma cruzi

Cofactor

Cofactor Comment Organism Structure
FAD
-
Crithidia fasciculata
FAD
-
Trypanosoma cruzi
NADPH
-
Crithidia fasciculata
NADPH
-
Trypanosoma cruzi