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Literature summary for 1.8.1.12 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)

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

Crystallization (Commentary)

Crystallization (Comment) Organism
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

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

KM Value [mM]

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

Molecular Weight [Da]

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

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei P39051
-
-

Purification (Commentary)

Purification (Comment) Organism
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)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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 ?
-
?
trypanothione + 5,5'-dithiobis-(2-nitrobenzoic acid)
-
Trypanosoma brucei trypanothione disulfide + thionitrobenzoate
-
?
trypanothione disulfide + NADPH + H+ highly specific for trypanothione disulfide Trypanosoma brucei trypanothione + NADP+
-
?

Subunits

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

Synonyms

Synonyms Comment Organism
trypanothione reductase
-
Trypanosoma brucei
TryR
-
Trypanosoma brucei

Turnover Number [1/s]

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

Cofactor

Cofactor Comment Organism Structure
FAD
-
Trypanosoma brucei
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

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

kcat/KM [mM/s]

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