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Literature summary for 1.8.1.12 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

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

Application

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

Inhibitors

Inhibitors Comment Organism Structure
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
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
melarsen-trypanothione disulfide-adduct
-
Crithidia fasciculata
melarsen-trypanothione disulfide-adduct
-
Trypanosoma brucei

KM Value [mM]

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

Natural Substrates/ Products (Substrates)

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

Organism

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
trypanothione disulfide + NADPH
-
Trypanosoma brucei trypanothione + NADP+
-
?
trypanothione disulfide + NADPH
-
Crithidia fasciculata trypanothione + NADP+
-
?
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
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

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

Ki Value [mM]

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