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Literature summary for 1.8.1.B1 extracted from

  • Kuntz Angela, N.; Davioud-Charvet, E.; Sayed Ahmed, A.; Califf Lindsay, L.; Dessolin, J.; Arner Elias, S.J.; Williams David, L.
    Thioredoxin glutathione reductase from Schistosoma mansoni: an essential parasite enzyme and a key drug target (2007), PLoS Med., 4, e206.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.8.1.B1

Application

Application Comment Organism
medicine TGR is a key target for antischistosomal drug development Schistosoma mansoni

Inhibitors

Inhibitors Comment Organism Structure
3-DAP 0.05 mM, complete inhibition Schistosoma mansoni
auranofin 0.05 mM, complete inhibition Schistosoma mansoni
aurothioglucose 0.05 mM, complete inhibition Schistosoma mansoni
aurothiomalate 0.05 mM, complete inhibition Schistosoma mansoni
CDE16-2 0.05 mM, 98% inhibition Schistosoma mansoni
CDE4 0.05 mM, 99% inhibition Schistosoma mansoni
JD159 0.05 mM, complete inhibition Schistosoma mansoni
LS826 0.05 mM, 95% inhibition Schistosoma mansoni
naphthazarin 0.05 mM, complete inhibition Schistosoma mansoni
OPZ 0.05 mM, 87% inhibition Schistosoma mansoni
PAT 0.05 mM, complete inhibition Schistosoma mansoni
RMA35 0.05 mM, 98% inhibition Schistosoma mansoni

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0137
-
 NADPH pH 7.4, 25°C Schistosoma mansoni
0.0715
-
 GSSG pH 7.4, 25°C Schistosoma mansoni
0.114
-
 5,5'-dithiobis(2-nitrobenzoic acid) pH 7.4, 25°C Schistosoma mansoni

Organism

Organism UniProt Comment Textmining
Schistosoma mansoni
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Schistosoma mansoni

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5,5'-dithiobis(2-nitrobenzoic acid) + NADPH + H+
-
 Schistosoma mansoni 2-nitro-5-thiobenzoate + NADP+
-
 ?
GSSG + NADPH + H+
-
 Schistosoma mansoni GSH + NADP+
-
 ?
thioredoxin + NADP+
-
 Schistosoma mansoni thioredoxin disulfide + NADPH
-
 ?

Synonyms

Synonyms Comment Organism
TGR
-
 Schistosoma mansoni

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
16
-
 5,5'-dithiobis(2-nitrobenzoic acid) pH 7.4, 25°C Schistosoma mansoni
20.1
-
 NADPH pH 7.4, 25°C Schistosoma mansoni
21.7
-
 GSSG pH 7.4, 25°C Schistosoma mansoni

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00001
-
 auranofin
-
 Schistosoma mansoni

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000007
-
 pH 7.4, 25°C, substrates: 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH Schistosoma mansoni auranofin
0.000009
-
 pH 7.4, 25°C, substrates: GSSG + NADPH Schistosoma mansoni auranofin
0.000037
-
 pH 7.4, 25°C, substrates: GSSG + NADPH Schistosoma mansoni PAT
0.00005
-
 pH 7.4, 25°C, substrates: GSSG + NADPH Schistosoma mansoni aurothiomalate
0.000051
-
 pH 7.4, 25°C, substrates: 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH Schistosoma mansoni PAT
0.00007
-
 pH 7.4, 25°C, substrates: 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH Schistosoma mansoni aurothioglucose
0.00009
-
 pH 7.4, 25°C, substrates: 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH Schistosoma mansoni aurothiomalate
0.0005
-
 pH 7.4, 25°C, substrates: 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH Schistosoma mansoni 3-DAP
0.0005
-
 pH 7.4, 25°C, substrates: 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH Schistosoma mansoni JD159
0.0005
-
 pH 7.4, 25°C, substrates: GSSG + NADPH Schistosoma mansoni CDE4
0.001
-
 pH 7.4, 25°C, substrates: GSSG + NADPH Schistosoma mansoni CDE16-2
0.001
-
 pH 7.4, 25°C, substrates: GSSG + NADPH Schistosoma mansoni JD159
0.0025
-
 pH 7.4, 25°C, substrates: 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH Schistosoma mansoni naphthazarin
0.003
-
 pH 7.4, 25°C, substrates: GSSG + NADPH Schistosoma mansoni aurothioglucose
0.004
-
 pH 7.4, 25°C, substrates: 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH Schistosoma mansoni RMA35
0.006
-
 pH 7.4, 25°C, substrates: GSSG + NADPH Schistosoma mansoni RMA35
0.007
-
 pH 7.4, 25°C, substrates: 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH Schistosoma mansoni CDE4
0.007
-
 pH 7.4, 25°C, substrates: GSSG + NADPH Schistosoma mansoni 3-DAP
0.008
-
 pH 7.4, 25°C, substrates: 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH Schistosoma mansoni LS826
0.008
-
 pH 7.4, 25°C, substrates: GSSG + NADPH Schistosoma mansoni LS826
0.01
-
 pH 7.4, 25°C, substrates: GSSG + NADPH Schistosoma mansoni naphthazarin
0.025
-
 pH 7.4, 25°C, substrates: 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH Schistosoma mansoni CDE16-2
0.05
-
 pH 7.4, 25°C, substrates: GSSG + NADPH Schistosoma mansoni OPZ
0.08
-
 pH 7.4, 25°C, substrates: 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH Schistosoma mansoni OPZ