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Literature summary extracted from

  • Holloway, G.A.; Charman, W.N.; Fairlamb, A.H.; Brun, R.; Kaiser, M.; Kostewicz, E.; Novello, P.M.; Parisot, J.P.; Richardson, J.; Street, I.P.; Watson, K.G.; Baell, J.B.
    Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity (2009), Antimicrob. Agents Chemother., 53, 2824-2833.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.8.1.12 (2Z)-2-[(2E)-2-(3H-indol-3-ylidene)ethylidene]-1-methyl-1,2-dihydroquinoline
-
 Trypanosoma cruzi
1.8.1.12 1-(1-benzylpiperidin-4-yl)-3-phenylthiourea
-
 Trypanosoma cruzi
1.8.1.12 1-(1-benzylpiperidin-4-yl)-3-pyridin-3-ylthiourea
-
 Trypanosoma cruzi
1.8.1.12 1-(1-phenylpiperidin-4-yl)-3-propylthiourea
-
 Trypanosoma cruzi
1.8.1.12 1-(2-phenoxyethyl)-3-[2-(piperidin-1-yl)ethyl]-1,3-dihydro-2H-benzimidazol-2-imine
-
 Trypanosoma cruzi
1.8.1.12 1-(4,6,8-trimethylquinazolin-2-yl)guanidine
-
 Trypanosoma cruzi
1.8.1.12 1-(4-methylquinazolin-2-yl)guanidine
-
 Trypanosoma cruzi
1.8.1.12 1-(methylsulfanyl)-4-[3-(methylsulfanyl)-1,2,4-triazin-5-yl]-5,6,7,8-tetrahydroisoquinoline
-
 Trypanosoma cruzi
1.8.1.12 1-phenyl-3-(1-phenylpiperidin-4-yl)thiourea
-
 Trypanosoma cruzi
1.8.1.12 1-phenyl-3-[1-(pyridin-3-yl)piperidin-4-yl]urea
-
 Trypanosoma cruzi
1.8.1.12 3-(methylsulfanyl)-5-phenyl-1,2,4-triazine
-
 Trypanosoma cruzi
1.8.1.12 3-cyano-1-azabicyclo[2.2.2]oct-3-yl acetate
-
 Trypanosoma cruzi
1.8.1.12 3-methoxy-3'-(methylsulfanyl)-5,5'-bi-1,2,4-triazine
-
 Trypanosoma cruzi
1.8.1.12 4,6,8-trimethyl-N-(4,4,6-trimethyl-1,4-dihydropyrimidin-2-yl)quinazolin-2-amine
-
 Trypanosoma cruzi
1.8.1.12 5,6-dimethyl-2-[(4,6,8-trimethylquinazolin-2-yl)amino]pyrimidin-4-ol
-
 Trypanosoma cruzi
1.8.1.12 7-ethoxy-4-methyl-N-(4,4,6-trimethyl-4,5-dihydropyrimidin-2-yl)quinazolin-2-amine
-
 Trypanosoma cruzi
1.8.1.12 7-ethyl-4-methyl-N-(4,4,6-trimethyl-4,5-dihydropyrimidin-2-yl)quinazolin-2-amine
-
 Trypanosoma cruzi
1.8.1.12 ajoene
-
 Trypanosoma cruzi
1.8.1.12 carmustine
-
 Trypanosoma cruzi
1.8.1.12 Mepacrine
-
 Trypanosoma cruzi
1.8.1.12 N-(4,6-dimethylpyrimidin-2-yl)-4,5,7-trimethylquinazolin-2-amine
-
 Trypanosoma cruzi
1.8.1.12 N-(4,6-dimethylpyrimidin-2-yl)-4,6-dimethylquinazolin-2-amine
-
 Trypanosoma cruzi
1.8.1.12 N-[(4-chlorophenyl)(phenyl)methoxy]-8-methyl-8-azabicyclo[3.2.1]octan-3-imine
-
 Trypanosoma cruzi
1.8.1.12 spermidine
-
 Trypanosoma cruzi
1.8.1.12 spermine
-
 Trypanosoma cruzi

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.8.1.12 0.0015
-
 trypanothione disulfide apparent value, in the presence of 0.05 mM DTNB and 0.15 mM NADPH, in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) BSA, and 0.05% (v/v) Tween 20, pH 7.5, at 22°C Trypanosoma cruzi

Organism

EC Number Organism UniProt Comment Textmining
1.8.1.12 Trypanosoma cruzi
-
-
-
1.8.1.12 Trypanosoma cruzi Silvio X10/1
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.8.1.12 trypanothione disulfide + NADPH + H+
-
 Trypanosoma cruzi trypanothione + NADP+
-
 ?
1.8.1.12 trypanothione disulfide + NADPH + H+
-
 Trypanosoma cruzi Silvio X10/1 trypanothione + NADP+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.8.1.12 trypanothione reductase
-
 Trypanosoma cruzi

Cofactor

EC Number Cofactor Comment Organism Structure
1.8.1.12 FAD
-
 Trypanosoma cruzi
1.8.1.12 NADPH
-
 Trypanosoma cruzi

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.8.1.12 0.002
-
 in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 1-(1-benzylpiperidin-4-yl)-3-phenylthiourea
1.8.1.12 0.009
-
 in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 1-(2-phenoxyethyl)-3-[2-(piperidin-1-yl)ethyl]-1,3-dihydro-2H-benzimidazol-2-imine
1.8.1.12 0.017
-
 in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 4,6,8-trimethyl-N-(4,4,6-trimethyl-1,4-dihydropyrimidin-2-yl)quinazolin-2-amine
1.8.1.12 0.023
-
 in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi (2Z)-2-[(2E)-2-(3H-indol-3-ylidene)ethylidene]-1-methyl-1,2-dihydroquinoline
1.8.1.12 0.027
-
 in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 3-methoxy-3'-(methylsulfanyl)-5,5'-bi-1,2,4-triazine
1.8.1.12 0.028
-
 in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 7-ethoxy-4-methyl-N-(4,4,6-trimethyl-4,5-dihydropyrimidin-2-yl)quinazolin-2-amine
1.8.1.12 0.032
-
 in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 7-ethyl-4-methyl-N-(4,4,6-trimethyl-4,5-dihydropyrimidin-2-yl)quinazolin-2-amine
1.8.1.12 0.033
-
 in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi N-[(4-chlorophenyl)(phenyl)methoxy]-8-methyl-8-azabicyclo[3.2.1]octan-3-imine
1.8.1.12 0.033
-
 in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 1-phenyl-3-(1-phenylpiperidin-4-yl)thiourea
1.8.1.12 0.052
-
 in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 3-cyano-1-azabicyclo[2.2.2]oct-3-yl acetate
1.8.1.12 0.1
-
 IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 1-(1-phenylpiperidin-4-yl)-3-propylthiourea
1.8.1.12 0.1
-
 IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 1-(1-benzylpiperidin-4-yl)-3-pyridin-3-ylthiourea
1.8.1.12 0.1
-
 IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 1-phenyl-3-[1-(pyridin-3-yl)piperidin-4-yl]urea
1.8.1.12 0.1
-
 IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 1-(methylsulfanyl)-4-[3-(methylsulfanyl)-1,2,4-triazin-5-yl]-5,6,7,8-tetrahydroisoquinoline
1.8.1.12 0.1
-
 IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 3-(methylsulfanyl)-5-phenyl-1,2,4-triazine
1.8.1.12 0.1
-
 IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 5,6-dimethyl-2-[(4,6,8-trimethylquinazolin-2-yl)amino]pyrimidin-4-ol
1.8.1.12 0.1
-
 IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi N-(4,6-dimethylpyrimidin-2-yl)-4,5,7-trimethylquinazolin-2-amine
1.8.1.12 0.1
-
 IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi N-(4,6-dimethylpyrimidin-2-yl)-4,6-dimethylquinazolin-2-amine
1.8.1.12 0.1
-
 IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 1-(4,6,8-trimethylquinazolin-2-yl)guanidine
1.8.1.12 0.1
-
 IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, 0.01% (v/v) bovine serum albumin, 0.05% (v/v) Tween 20, pH 7.5, 22°C Trypanosoma cruzi 1-(4-methylquinazolin-2-yl)guanidine