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Literature summary for 6.3.1.9 extracted from
- Cloning, expression, characterization and inhibition studies on trypanothione synthetase, a drug target enzyme, from Leishmania donovani (2011), Biol. Chem., 392, 1113-1122.
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | trypanothione synthetase is a validated drug target | Leishmania donovani |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of His-tagged enzyme in Escherichia coli strain BL21 star (DE3) | Leishmania donovani |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| betulin | competitive inhibition | Leishmania donovani |  |
| conessine | competitive allosteric inhibition | Leishmania donovani | |
| glutathione | substrate inhibition | Leishmania donovani | |
| tomatine | competitive inhibition versus spermidine, uncompetitive inhibition with respect to ATP and GSH | Leishmania donovani | |
| uvaol | competitive allosteric inhibition | Leishmania donovani | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | Michaelis-Menten kinetics, simple hyperbolic kinetics with fixed glutathione concentration and with other substrates limiting Km values for Mg2+ | Leishmania donovani | |
| 0.0142 | - |
ATP | pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | |
| 0.0332 | - |
glutathione | pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | |
| 0.1396 | - |
spermidine | pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | required | Leishmania donovani | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 74500 | - |
x * 74500, recombinant detagged enzyme, SDS-PAGE | Leishmania donovani |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| glutathione + spermidine + 2 ATP | Leishmania donovani | - |
N1,N8-bis(glutathionyl)spermidine + 2 ADP + 2 phosphate | - |
? | |
| glutathione + spermidine + 2 ATP | Leishmania donovani UR6 | - |
N1,N8-bis(glutathionyl)spermidine + 2 ADP + 2 phosphate | - |
? | |
| additional information | Leishmania donovani | trypanothione synthetase synthesizes trypanothione from glutathione and spermidine | ? | - |
? | |
| additional information | Leishmania donovani UR6 | trypanothione synthetase synthesizes trypanothione from glutathione and spermidine | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Leishmania donovani | G5D5D5 | - |
- |
| Leishmania donovani UR6 | G5D5D5 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant His-tagged enzyme from Escherichia coli strain BL21 star (DE3) by nickel affinity chromatography and tag cleavage through thrombin | Leishmania donovani |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| promastigote | - |
Leishmania donovani | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| glutathione + spermidine + 2 ATP | - |
Leishmania donovani | N1,N8-bis(glutathionyl)spermidine + 2 ADP + 2 phosphate | - |
? | |
| glutathione + spermidine + 2 ATP | - |
Leishmania donovani UR6 | N1,N8-bis(glutathionyl)spermidine + 2 ADP + 2 phosphate | - |
? | |
| additional information | trypanothione synthetase synthesizes trypanothione from glutathione and spermidine | Leishmania donovani | ? | - |
? | |
| additional information | trypanothione synthetase synthesizes trypanothione from glutathione and spermidine | Leishmania donovani UR6 | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| ? | x * 74500, recombinant detagged enzyme, SDS-PAGE | Leishmania donovani |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Trypanothione synthetase | - |
Leishmania donovani |
| TryS | - |
Leishmania donovani |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 25 | - |
- |
Leishmania donovani |
Temperature Range [°C]
| Temperature Minimum [°C] | Temperature Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 10 | 60 | residual activity above | Leishmania donovani |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 1.3 | - |
glutathione | pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8 | - |
- |
Leishmania donovani |
pH Range
| pH Minimum | pH Maximum | Comment | Organism |
|---|---|---|---|
| 5 | 11 | inactive above or below | Leishmania donovani |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Leishmania donovani | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | inhibition kinetics, overview | Leishmania donovani | |
| 0.0031 | - |
conessine | pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | |
| 0.0036 | - |
uvaol | pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | |
| 0.0063 | - |
betulin | pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | |
| 0.0068 | - |
tomatine | versus GSH, pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | |
| 0.0125 | - |
tomatine | pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | |
| 0.866 | - |
glutathione | pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0112 | - |
pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | uvaol | |
| 0.0117 | - |
pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | betulin | |
| 0.0134 | - |
pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | conessine | |
| 0.018 | - |
pH 8.0, 25°C, recombinant enzyme | Leishmania donovani | tomatine | |
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