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Literature summary for 6.3.1.9 extracted from

  • Benitez, D.; Medeiros, A.; Fiestas, L.; Panozzo-Zenere, E.A.; Maiwald, F.; Prousis, K.C.; Roussaki, M.; Calogeropoulou, T.; Detsi, A.; Jaeger, T.; Sarlauskas, J.; Peterlin Masic, L.; Kunick, C.; Labadie, G.R.; Flohe, L.; Comini, M.A.
    Identification of novel chemical scaffolds inhibiting trypanothione synthetase from pathogenic trypanosomatids (2016), PLoS Negl. Trop. Dis., 10, e0004617 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 6.3.1.9

Activating Compound

Activating Compound Comment Organism Structure
1,4,7-trioxo-1lambda5,4lambda5,7lambda5-benzo[1,2-c:3,4-c':5,6-c'']tris[1,2,5]oxadiazole activates, 118.8% activity Trypanosoma brucei brucei
1-(1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one activates, 107.1% activity Trypanosoma cruzi
1-(1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one activates, 166.3% activity Trypanosoma brucei brucei
1-(1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-5-(4-fluorophenyl)-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one activates, 126.7% activity Trypanosoma brucei brucei
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-hydroxy-3-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one activates, 119.1% activity Trypanosoma brucei brucei
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one activates, 119.0% activity Trypanosoma brucei brucei
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(3,4-dimethoxybenzoyl)-5-(4-fluorophenyl)-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one activates, 123.2% activity Trypanosoma brucei brucei
4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-1-(6-methoxy-1,3-benzothiazol-2-yl)-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one activates, 116.4% activity Trypanosoma brucei brucei
4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1-(6-methyl-1,3-benzothiazol-2-yl)-1,5-dihydro-2H-pyrrol-2-one activates, 109.7% activity Trypanosoma cruzi
4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1-(6-methyl-1,3-benzothiazol-2-yl)-1,5-dihydro-2H-pyrrol-2-one activates, 128.2% activity Trypanosoma brucei brucei
6-fluoro-3-oxo-4,5-didehydro-2,1,3lambda5-benzoxadiazole activates, 118.8% activity Trypanosoma cruzi
8-[(2E)-2-[(2,4-dihydroxyphenyl)methylidene]hydrazinyl]-7-(2-hydroxy-3-phenoxypropyl)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione activates, 161.6% activity Trypanosoma cruzi
J20 slightly stimulating Leishmania infantum
additional information no effect by 1H-purine-2,6(3H,7H)-dione derivatives (Z)-8-(2-(2,4-dihydroxybenzylidene)hydrazinyl)-7-(2-hydroxy-3-phenoxy propyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione and 6-fluoro-3-oxo-4,5-didehydro-2,1,3lambda5-benzoxadiazole Trypanosoma brucei brucei
[3-[4-([6-(3,4-dimethoxyphenyl)-7-[(ethylcarbamothioyl)amino]pyrido[2,3-d]pyrimidin-2-yl]amino)phenyl]propyl]molybdenum(1+) activates, 168.6% activity Trypanosoma cruzi

Cloned(Commentary)

Cloned (Comment) Organism
gene TRS, recombinant expression of N-terminally His-tagged enzyme in Escherichia coli strains BL21(DE3) or Tuner (DE3) Trypanosoma cruzi
gene tryS, recombinant expression of N-terminally His-tagged enzyme in Escherichia coli strains BL21(DE3) or Tuner (DE3) Leishmania infantum
gene tryS, recombinant expression of N-terminally His-tagged enzyme in Escherichia coli strains BL21(DE3) or Tuner (DE3) Trypanosoma brucei brucei

Inhibitors

Inhibitors Comment Organism Structure
(Z)-8-(2-(2,4-dihydroxybenzylidene)hydrazinyl)-7-(2-hydroxy-3-phenoxy propyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione 88.5% activity remaining Leishmania infantum
1,4,7-trioxo-1lambda5,4lambda5,7lambda5-benzo[1,2-c:3,4-c':5,6-c'']tris[1,2,5]oxadiazole 64.4% activity remaining Trypanosoma cruzi
1-(1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one 83.5% activity remaining Leishmania infantum
1-(1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-5-(4-fluorophenyl)-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one 83.5% activity remaining Leishmania infantum
1-(1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-5-(4-fluorophenyl)-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one 90.8% activity remaining Trypanosoma cruzi
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-hydroxy-3-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one 85.3% activity remaining Leishmania infantum
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-hydroxy-3-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one 97.4% activity remaining Trypanosoma cruzi
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one 82.1% activity remaining Leishmania infantum
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one 98.7% activity remaining Trypanosoma cruzi
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(3,4-dimethoxybenzoyl)-5-(4-fluorophenyl)-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one 66.0% activity remaining Leishmania infantum
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(3,4-dimethoxybenzoyl)-5-(4-fluorophenyl)-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one 99.6% activity remaining Trypanosoma cruzi
2-(9-bromo-3-chloro-6-oxo-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl)-N-[2-(methylamino)ethyl]acetamide
-
 Leishmania infantum
2-(9-bromo-3-chloro-6-oxo-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl)-N-[2-(methylamino)ethyl]acetamide 59.0% activity remaining Trypanosoma brucei brucei
2-(9-bromo-3-chloro-6-oxo-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl)-N-[2-(methylamino)ethyl]acetamide 55.5% activity remaining Trypanosoma cruzi
4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-1-(6-methoxy-1,3-benzothiazol-2-yl)-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one 77.9% activity remaining Leishmania infantum
4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-1-(6-methoxy-1,3-benzothiazol-2-yl)-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one 97.6% activity remaining Trypanosoma cruzi
4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1-(6-methyl-1,3-benzothiazol-2-yl)-1,5-dihydro-2H-pyrrol-2-one 83.9% activity remaining Leishmania infantum
5-oxo-1H,3H-5lambda5-benzo[1,2-c:4,5-c']bis[1,2,5]oxadiazole
-
 Leishmania infantum
5-oxo-1H,3H-5lambda5-benzo[1,2-c:4,5-c']bis[1,2,5]oxadiazole 7.3% activity remaining Trypanosoma brucei brucei
5-oxo-1H,3H-5lambda5-benzo[1,2-c:4,5-c']bis[1,2,5]oxadiazole 63.5% activity remaining Trypanosoma cruzi
6-fluoro-3-oxo-4,5-didehydro-2,1,3lambda5-benzoxadiazole 84.1% activity remaining Leishmania infantum
GSH substrate inhibition Trypanosoma brucei brucei
additional information screening of different scaffold-derived compounds for inhibitory activity on enzyme TryS, overview. No inhibition by [3-[4-([6-(3,4-dimethoxyphenyl)-7-[(ethylcarbamothioyl)amino]pyrido[2,3-d]pyrimidin-2-yl]amino)phenyl]propyl]molybdenum(1+) and 1,4,7-trioxo-1lambda5,4lambda5,7lambda5-benzo[1,2-c:3,4-c':5,6-c'']tris[1,2,5]oxadiazole Leishmania infantum
additional information screening of different scaffold-derived compounds for inhibitory activity on enzyme TryS, overview. No effect by 8-[(2E)-2-[(2,4-dihydroxyphenyl)methylidene]hydrazinyl]-7-(2-hydroxy-3-phenoxypropyl)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione and J31 Trypanosoma brucei brucei
additional information screening of different scaffold-derived compounds for inhibitory activity on enzyme TryS, overview Trypanosoma cruzi
N,N'-[6-(2,5-dichlorophenyl)pyrido[2,3-d]pyrimidine-2,7-diyl]bis(N'-tert-butylurea)
-
 Leishmania infantum
N,N'-[6-(2,5-dichlorophenyl)pyrido[2,3-d]pyrimidine-2,7-diyl]bis(N'-tert-butylurea) 24.3% activity remaining Trypanosoma brucei brucei
N,N'-[6-(2,5-dichlorophenyl)pyrido[2,3-d]pyrimidine-2,7-diyl]bis(N'-tert-butylurea) 61.3% activity remaining Trypanosoma cruzi
N,N'-[6-(2H-1,3-benzodioxol-5-yl)pyrido[2,3-d]pyrimidine-2,7-diyl]bis(N'-tert-butylurea)
-
 Leishmania infantum
N,N'-[6-(2H-1,3-benzodioxol-5-yl)pyrido[2,3-d]pyrimidine-2,7-diyl]bis(N'-tert-butylurea) 25.3% activity remaining Trypanosoma brucei brucei
N,N'-[6-(2H-1,3-benzodioxol-5-yl)pyrido[2,3-d]pyrimidine-2,7-diyl]bis(N'-tert-butylurea) 52.2% activity remaining Trypanosoma cruzi
N-[2-(methylamino)ethyl]-2-[6-oxo-9-(trifluoromethyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl]acetamide i.e. FS-554 Leishmania infantum
N-[2-(methylamino)ethyl]-2-[6-oxo-9-(trifluoromethyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl]acetamide i.e. FS-554 Trypanosoma brucei brucei
N-[2-(methylamino)ethyl]-2-[6-oxo-9-(trifluoromethyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl]acetamide i.e. FS-554, 40.5% activity remaining Trypanosoma cruzi
N-[2-amino-6-(2H-1,3-benzodioxol-5-yl)pyrido[2,3-d]pyrimidin-7-yl]-N'-ethylthiourea
-
 Leishmania infantum
N-[2-amino-6-(2H-1,3-benzodioxol-5-yl)pyrido[2,3-d]pyrimidin-7-yl]-N'-ethylthiourea 20.9% activity remaining Trypanosoma brucei brucei
N-[2-amino-6-(2H-1,3-benzodioxol-5-yl)pyrido[2,3-d]pyrimidin-7-yl]-N'-ethylthiourea 65.4% activity remaining Trypanosoma cruzi
N-[2-amino-6-(naphthalen-2-yl)pyrido[2,3-d]pyrimidin-7-yl]-N'-tert-butylurea
-
 Leishmania infantum
N-[2-amino-6-(naphthalen-2-yl)pyrido[2,3-d]pyrimidin-7-yl]-N'-tert-butylurea 48.7% activity remaining Trypanosoma brucei brucei
N-[2-amino-6-(naphthalen-2-yl)pyrido[2,3-d]pyrimidin-7-yl]-N'-tert-butylurea 32.3% activity remaining Trypanosoma cruzi
N1,N10-bis[[4-(propan-2-yl)phenyl]methyl]decane-1,10-diamine
-
 Leishmania infantum
N1,N10-bis[[4-(propan-2-yl)phenyl]methyl]decane-1,10-diamine 51.1% activity remaining Trypanosoma brucei brucei
N1,N10-bis[[4-(propan-2-yl)phenyl]methyl]decane-1,10-diamine 53.5% activity remaining Trypanosoma cruzi
N1,N12-bis[(4-bromophenyl)methyl]dodecane-1,12-diamine
-
 Leishmania infantum
N1,N12-bis[(4-bromophenyl)methyl]dodecane-1,12-diamine 47.5% activity remaining Trypanosoma brucei brucei
N1,N12-bis[(4-bromophenyl)methyl]dodecane-1,12-diamine 30.8% activity remaining Trypanosoma cruzi
N1,N12-bis[(4-chlorophenyl)methyl]dodecane-1,12-diamine
-
 Leishmania infantum
N1,N12-bis[(4-chlorophenyl)methyl]dodecane-1,12-diamine 42.4% activity remaining Trypanosoma brucei brucei
N1,N12-bis[(4-chlorophenyl)methyl]dodecane-1,12-diamine 23.8% activity remaining Trypanosoma cruzi
N1,N3-bis[(4-methoxyphenyl)methyl]propane-1,3-diamine
-
 Trypanosoma cruzi
N1,N4-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]butane-1,4-diamine
-
 Leishmania infantum
N1,N4-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]butane-1,4-diamine 50.9% activity remaining Trypanosoma brucei brucei
N1,N4-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]butane-1,4-diamine 25.6% activity remaining Trypanosoma cruzi
N1,N4-bis[[4-(benzyloxy)phenyl]methyl]butane-1,4-diamine
-
 Leishmania infantum
N1,N4-bis[[4-(benzyloxy)phenyl]methyl]butane-1,4-diamine 37.9% activity remaining Trypanosoma brucei brucei
N1,N4-bis[[4-(benzyloxy)phenyl]methyl]butane-1,4-diamine 26.6% activity remaining Trypanosoma cruzi
N1,N6-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]hexane-1,6-diamine
-
 Leishmania infantum
N1,N6-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]hexane-1,6-diamine 61.2% activity remaining Trypanosoma brucei brucei
N1,N6-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]hexane-1,6-diamine 17.0% activity remaining Trypanosoma cruzi
N1,N6-bis[[4-(benzyloxy)phenyl]methyl]hexane-1,6-diamine
-
 Leishmania infantum
N1,N6-bis[[4-(benzyloxy)phenyl]methyl]hexane-1,6-diamine 48.9% activity remaining Trypanosoma brucei brucei
N1,N6-bis[[4-(benzyloxy)phenyl]methyl]hexane-1,6-diamine 33.4% activity remaining Trypanosoma cruzi
N1,N8-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]octane-1,8-diamine
-
 Leishmania infantum
N1,N8-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]octane-1,8-diamine 55.6% activity remaining Trypanosoma brucei brucei
N1,N8-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]octane-1,8-diamine 28.9% activity remaining Trypanosoma cruzi
[3-[4-([6-(3,4-dimethoxyphenyl)-7-[(ethylcarbamothioyl)amino]pyrido[2,3-d]pyrimidin-2-yl]amino)phenyl]propyl]molybdenum(1+) 81.3% activity remaining Trypanosoma brucei brucei

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information Michaelis-Menten steady-state kinetics Trypanosoma cruzi
additional information
-
 additional information Michaelis-Menten steady-state kinetics Leishmania infantum
additional information
-
 additional information Michaelis-Menten steady-state kinetics Trypanosoma brucei brucei

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Trypanosoma cruzi
Mg2+ required Leishmania infantum
Mg2+ required Trypanosoma brucei brucei

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
glutathione + glutathionylspermidine + ATP Trypanosoma cruzi
-
 N1,N8-bis(glutathionyl)spermidine + ADP + phosphate
-
 ?
glutathione + glutathionylspermidine + ATP Leishmania infantum
-
 N1,N8-bis(glutathionyl)spermidine + ADP + phosphate
-
 ?
glutathione + glutathionylspermidine + ATP Trypanosoma brucei brucei
-
 N1,N8-bis(glutathionyl)spermidine + ADP + phosphate
-
 ?
glutathione + glutathionylspermidine + ATP Trypanosoma cruzi CL Brener
-
 N1,N8-bis(glutathionyl)spermidine + ADP + phosphate
-
 ?
glutathione + glutathionylspermidine + ATP Trypanosoma brucei brucei 427
-
 N1,N8-bis(glutathionyl)spermidine + ADP + phosphate
-
 ?
glutathione + glutathionylspermidine + ATP Leishmania infantum JPCM5 /MHOM / MA / 67 / ITMAP263
-
 N1,N8-bis(glutathionyl)spermidine + ADP + phosphate
-
 ?
glutathione + spermidine + ATP Trypanosoma cruzi
-
 glutathionylspermidine + ADP + phosphate
-
 ?
glutathione + spermidine + ATP Leishmania infantum
-
 glutathionylspermidine + ADP + phosphate
-
 ?
glutathione + spermidine + ATP Trypanosoma brucei brucei
-
 glutathionylspermidine + ADP + phosphate
-
 ?
glutathione + spermidine + ATP Trypanosoma cruzi CL Brener
-
 glutathionylspermidine + ADP + phosphate
-
 ?
glutathione + spermidine + ATP Trypanosoma brucei brucei 427
-
 glutathionylspermidine + ADP + phosphate
-
 ?
glutathione + spermidine + ATP Leishmania infantum JPCM5 /MHOM / MA / 67 / ITMAP263
-
 glutathionylspermidine + ADP + phosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Leishmania infantum A4I2Z3
-
-
Leishmania infantum JPCM5 /MHOM / MA / 67 / ITMAP263 A4I2Z3
-
-
Trypanosoma brucei brucei Q8IEX1 cell line 514-1313
-
Trypanosoma brucei brucei 427 Q8IEX1 cell line 514-1313
-
Trypanosoma cruzi Q9GT49
-
-
Trypanosoma cruzi CL Brener Q9GT49
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged enzyme from Escherichia coli strains BL21(DE3) or Tuner (DE3) by affinity chromatography Trypanosoma cruzi
recombinant His-tagged enzyme from Escherichia coli strains BL21(DE3) or Tuner (DE3) by affinity chromatography Leishmania infantum
recombinant His-tagged enzyme from Escherichia coli strains BL21(DE3) or Tuner (DE3) by affinity chromatography Trypanosoma brucei brucei

Source Tissue

Source Tissue Comment Organism Textmining
promastigote
-
 Leishmania infantum
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glutathione + glutathionylspermidine + ATP
-
 Trypanosoma cruzi N1,N8-bis(glutathionyl)spermidine + ADP + phosphate
-
 ?
glutathione + glutathionylspermidine + ATP
-
 Leishmania infantum N1,N8-bis(glutathionyl)spermidine + ADP + phosphate
-
 ?
glutathione + glutathionylspermidine + ATP
-
 Trypanosoma brucei brucei N1,N8-bis(glutathionyl)spermidine + ADP + phosphate
-
 ?
glutathione + glutathionylspermidine + ATP
-
 Trypanosoma cruzi CL Brener N1,N8-bis(glutathionyl)spermidine + ADP + phosphate
-
 ?
glutathione + glutathionylspermidine + ATP
-
 Trypanosoma brucei brucei 427 N1,N8-bis(glutathionyl)spermidine + ADP + phosphate
-
 ?
glutathione + glutathionylspermidine + ATP
-
 Leishmania infantum JPCM5 /MHOM / MA / 67 / ITMAP263 N1,N8-bis(glutathionyl)spermidine + ADP + phosphate
-
 ?
glutathione + spermidine + ATP
-
 Trypanosoma cruzi glutathionylspermidine + ADP + phosphate
-
 ?
glutathione + spermidine + ATP
-
 Leishmania infantum glutathionylspermidine + ADP + phosphate
-
 ?
glutathione + spermidine + ATP
-
 Trypanosoma brucei brucei glutathionylspermidine + ADP + phosphate
-
 ?
glutathione + spermidine + ATP
-
 Trypanosoma cruzi CL Brener glutathionylspermidine + ADP + phosphate
-
 ?
glutathione + spermidine + ATP
-
 Trypanosoma brucei brucei 427 glutathionylspermidine + ADP + phosphate
-
 ?
glutathione + spermidine + ATP
-
 Leishmania infantum JPCM5 /MHOM / MA / 67 / ITMAP263 glutathionylspermidine + ADP + phosphate
-
 ?

Synonyms

Synonyms Comment Organism
LiTRYS
-
 Leishmania infantum
TbTryS
-
 Trypanosoma brucei brucei
TcTryS
-
 Trypanosoma cruzi
TRS
-
 Trypanosoma cruzi
TryS
-
 Trypanosoma cruzi
TryS
-
 Leishmania infantum
TryS
-
 Trypanosoma brucei brucei
tyrS
-
 Trypanosoma brucei brucei

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
 assay at room temperature Trypanosoma cruzi
22
-
 assay at room temperature Leishmania infantum
22
-
 assay at room temperature Trypanosoma brucei brucei

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Trypanosoma cruzi
7.4
-
 assay at Leishmania infantum
7.4
-
 assay at Trypanosoma brucei brucei

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Trypanosoma cruzi
ATP
-
 Leishmania infantum
ATP
-
 Trypanosoma brucei brucei

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00015
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum 2-(9-bromo-3-chloro-6-oxo-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl)-N-[2-(methylamino)ethyl]acetamide
0.00035
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N-[2-(methylamino)ethyl]-2-[6-oxo-9-(trifluoromethyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl]acetamide
0.0136
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N-[2-amino-6-(2H-1,3-benzodioxol-5-yl)pyrido[2,3-d]pyrimidin-7-yl]-N'-ethylthiourea
0.0138
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N,N'-[6-(2,5-dichlorophenyl)pyrido[2,3-d]pyrimidine-2,7-diyl]bis(N'-tert-butylurea)
0.0153
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N,N'-[6-(2H-1,3-benzodioxol-5-yl)pyrido[2,3-d]pyrimidine-2,7-diyl]bis(N'-tert-butylurea)
0.0234
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N1,N4-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]butane-1,4-diamine
0.0259
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N1,N12-bis[(4-bromophenyl)methyl]dodecane-1,12-diamine
0.0263
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N1,N6-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]hexane-1,6-diamine
0.0313
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum 5-oxo-1H,3H-5lambda5-benzo[1,2-c:4,5-c']bis[1,2,5]oxadiazole
0.0321
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N-[2-amino-6-(naphthalen-2-yl)pyrido[2,3-d]pyrimidin-7-yl]-N'-tert-butylurea
0.0391
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N1,N6-bis[[4-(benzyloxy)phenyl]methyl]hexane-1,6-diamine
0.0478
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N1,N10-bis[[4-(propan-2-yl)phenyl]methyl]decane-1,10-diamine
0.0496
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N1,N8-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]octane-1,8-diamine
0.0515
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N1,N12-bis[(4-chlorophenyl)methyl]dodecane-1,12-diamine
0.0567
-
 pH 7.4, 22°C, recombinant enzyme Leishmania infantum N1,N4-bis[[4-(benzyloxy)phenyl]methyl]butane-1,4-diamine

General Information

General Information Comment Organism
metabolism trypanothione dependent redox metabolism, overview. Trypanothione synthetase catalyzes the ligation of two molecules of gluthatione to one of spermidine using the energy provided by two ATP molecules. Trypanothione reductase maintains trypanothione in the reduced state at expenses of NADPH, which can be supplied by the oxidative phase of the pentose phosphate pathway via glucose 6-phosphate dehydrogenase Trypanosoma cruzi
metabolism trypanothione dependent redox metabolism, overview. Trypanothione synthetase catalyzes the ligation of two molecules of gluthatione to one of spermidine using the energy provided by two ATP molecules. Trypanothione reductase maintains trypanothione in the reduced state at expenses of NADPH, which can be supplied by the oxidative phase of the pentose phosphate pathway via glucose 6-phosphate dehydrogenase Leishmania infantum
metabolism trypanothione dependent redox metabolism, overview. Trypanothione synthetase catalyzes the ligation of two molecules of gluthatione to one of spermidine using the energy provided by two ATP molecules. Trypanothione reductase maintains trypanothione in the reduced state at expenses of NADPH, which can be supplied by the oxidative phase of the pentose phosphate pathway via glucose 6-phosphate dehydrogenase Trypanosoma brucei brucei
physiological function in pathogenic trypanosomatids, a single enzyme, trypanothione synthetase (TryS), catalyzes trypanothione biosynthesis, which is indispensable for parasite survival. Reduced trypanothione is involved in multiple functions such as the detoxification of xenobiotics, cell proliferation, defense against oxidants and protein thiol-redox homeostasis Trypanosoma cruzi
physiological function in pathogenic trypanosomatids, a single enzyme, trypanothione synthetase (TryS), catalyzes trypanothione biosynthesis, which is indispensable for parasite survival. Reduced trypanothione is involved in multiple functions such as the detoxification of xenobiotics, cell proliferation, defense against oxidants and protein thiol-redox homeostasis Leishmania infantum
physiological function in pathogenic trypanosomatids, a single enzyme, trypanothione synthetase (TryS), catalyzes trypanothione biosynthesis, which is indispensable for parasite survival. Reduced trypanothione is involved in multiple functions such as the detoxification of xenobiotics, cell proliferation, defense against oxidants and protein thiol-redox homeostasis Trypanosoma brucei brucei