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Literature summary extracted from

  • Fairlamb, A.H.; Henderson, G.B.; Cerami, A.
    Trypanothione is the primary target for arsenical drugs against African trypanosomes (1989), Proc. Natl. Acad. Sci. USA, 86, 2607-2611.
    View publication on PubMedView publication on EuropePMC

Activating Compound

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

Application

EC Number Application Comment Organism
1.8.1.12 medicine
-
 Crithidia fasciculata
1.8.1.12 medicine enzyme substrate trypanothione disulfide is the primary target for arsenical drugs against african trypanosomes Trypanosoma brucei

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.8.1.12 melarsen-trypanothione disulfide adduct i.e. adduct of p-(4,6-diamino-S-triazinyl-2-yl)aminophenyl arsenoxide with N1,N8-bis-(glutathionyl)spermidine Crithidia fasciculata
1.8.1.12 melarsen-trypanothione disulfide adduct i.e. adduct of p-(4,6-diamino-S-triazinyl-2-yl)aminophenyl arsenoxide with N1,N8-bis-(glutathionyl)spermidine Trypanosoma brucei
1.8.1.12 melarsen-trypanothione disulfide-adduct
-
 Crithidia fasciculata
1.8.1.12 melarsen-trypanothione disulfide-adduct
-
 Trypanosoma brucei

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.8.1.12 0.053
-
 trypanothione disulfide
-
 Crithidia fasciculata
1.8.1.12 0.058
-
 trypanothione disulfide
-
 Trypanosoma brucei

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
1.8.1.12 Crithidia fasciculata
-
 insect-parasitic trypanosomatid
-
1.8.1.12 Trypanosoma brucei
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.8.1.12 trypanothione disulfide + NADPH
-
 Trypanosoma brucei trypanothione + NADP+
-
 ?
1.8.1.12 trypanothione disulfide + NADPH
-
 Crithidia fasciculata trypanothione + NADP+
-
 ?
1.8.1.12 trypanothione disulfide + NADPH trypanothione is the oxidized form of N1,N8-bis-(glutathionyl)spermidine, the latter form a stable adduct with melarsen oxide Trypanosoma brucei trypanothione + NADP+
-
 r
1.8.1.12 trypanothione disulfide + NADPH trypanothione is the oxidized form of N1,N8-bis-(glutathionyl)spermidine, the latter form a stable adduct with melarsen oxide Crithidia fasciculata trypanothione + NADP+
-
 r

Cofactor

EC Number Cofactor Comment Organism Structure
1.8.1.12 FAD
-
 Trypanosoma brucei
1.8.1.12 FAD
-
 Crithidia fasciculata
1.8.1.12 NADPH
-
 Trypanosoma brucei
1.8.1.12 NADPH
-
 Crithidia fasciculata

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.8.1.12 0.009
-
 melarsen-trypanothione disulfide-adduct
-
 Trypanosoma brucei
1.8.1.12 0.036
-
 melarsen-trypanothione disulfide-adduct
-
 Crithidia fasciculata