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Literature summary extracted from

  • Jones, D.C.; Ariza, A.; Chow, W.H.; Oza, S.L.; Fairlamb, A.H.
    Comparative structural, kinetic and inhibitor studies of Trypanosoma brucei trypanothione reductase with T. cruzi (2010), Mol. Biochem. Parasitol., 169, 12-19.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.8.1.12 expressed in Escherichia coli BL21 Star (DE3)pLysS cells Trypanosoma brucei

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.8.1.12 hanging drop vapor diffusion method, using 0.1 M bis-Tris propane pH 8.0, 5% (v/v) PEG 400, 2M ammonium sulfate Trypanosoma brucei

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.8.1.12 1-(3,4-dichlorophenyl)-3-(dimethylamino)propan-1-one
-
 Trypanosoma brucei
1.8.1.12 3-(dimethylamino)-1-(3-nitrophenyl)propan-1-one
-
 Trypanosoma brucei
1.8.1.12 3-(dimethylamino)-1-[4-(methylsulfonyl)phenyl]propan-1-one
-
 Trypanosoma brucei
1.8.1.12 4-[[bis(2-hydroxyethyl)amino]methyl]-2,6-dibutylphenol
-
 Trypanosoma brucei
1.8.1.12 citalopram
-
 Trypanosoma brucei
1.8.1.12 clomipramine
-
 Trypanosoma brucei
1.8.1.12 ebselen
-
 Trypanosoma brucei
1.8.1.12 Quinacrine
-
 Trypanosoma brucei
1.8.1.12 thioridazine
-
 Trypanosoma brucei
1.8.1.12 Trifluoperazine
-
 Trypanosoma brucei

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.8.1.12 0.00077
-
 NADPH in 40 mM HEPES, pH 7.4, 1 mM EDTA Trypanosoma brucei
1.8.1.12 0.0069
-
 trypanothione disulfide in 40 mM HEPES, pH 7.4, 1 mM EDTA Trypanosoma brucei

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
1.8.1.12 48000
-
 2 * 48000, gel filtration Trypanosoma brucei
1.8.1.12 53160
-
 subunit, calculated from amino acid sequence Trypanosoma brucei
1.8.1.12 93000
-
 analytical ultracentrifugation Trypanosoma brucei
1.8.1.12 96000
-
 gel filtration Trypanosoma brucei

Organism

EC Number Organism UniProt Comment Textmining
1.8.1.12 Trypanosoma brucei P39051
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.8.1.12 recombinant enzyme is purified by ammonium sulfate precipitation, 2'5'-ADP Sepharose affinity column chromatography, and anion exchange chromatography Trypanosoma brucei

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.8.1.12 additional information the rate of reduction of 0.05 mM glutathione disulfide is 0.03% of that obtained with 0.05 mM trypanothione disulfide Trypanosoma brucei ?
-
 ?
1.8.1.12 trypanothione + 5,5'-dithiobis-(2-nitrobenzoic acid)
-
 Trypanosoma brucei trypanothione disulfide + thionitrobenzoate
-
 ?
1.8.1.12 trypanothione disulfide + NADPH + H+ highly specific for trypanothione disulfide Trypanosoma brucei trypanothione + NADP+
-
 ?

Subunits

EC Number Subunits Comment Organism
1.8.1.12 homodimer 2 * 48000, gel filtration Trypanosoma brucei

Synonyms

EC Number Synonyms Comment Organism
1.8.1.12 trypanothione reductase
-
 Trypanosoma brucei
1.8.1.12 TryR
-
 Trypanosoma brucei

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.8.1.12 46.8
-
 trypanothione disulfide in 40 mM HEPES, pH 7.4, 1 mM EDTA Trypanosoma brucei

Cofactor

EC Number Cofactor Comment Organism Structure
1.8.1.12 FAD
-
 Trypanosoma brucei
1.8.1.12 NADPH highly specific for NADPH, activity with 0.15 mM NADH is only 5.7% of that obtained with 0.15 mM NADPH Trypanosoma brucei

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.8.1.12 0.00018
-
 in 40 mM HEPES, pH 7.4, 1 mM EDTA Trypanosoma brucei ebselen
1.8.1.12 0.00958
-
 in 40 mM HEPES, pH 7.4, 1 mM EDTA Trypanosoma brucei thioridazine
1.8.1.12 0.0111
-
 in 40 mM HEPES, pH 7.4, 1 mM EDTA Trypanosoma brucei clomipramine
1.8.1.12 0.0221
-
 in 40 mM HEPES, pH 7.4, 1 mM EDTA Trypanosoma brucei Quinacrine
1.8.1.12 0.0405
-
 in 40 mM HEPES, pH 7.4, 1 mM EDTA Trypanosoma brucei Trifluoperazine
1.8.1.12 0.0823
-
 in 40 mM HEPES, pH 7.4, 1 mM EDTA Trypanosoma brucei citalopram

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
1.8.1.12 6782
-
 trypanothione disulfide in 40 mM HEPES, pH 7.4, 1 mM EDTA Trypanosoma brucei