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Literature summary extracted from
- Mechanism of inhibition of trypanothione reductase and glutathione reductase by trivalent organic arsenicals (1994), Eur. J. Biochem., 221, 285-295.
Activating Compound
| EC Number | Activating Compound | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.8.1.7 | FAD analogues | - |
Homo sapiens | |
| 1.8.1.12 | additional information | activity is dependent on a redox-active cysteine at the active centre | Crithidia fasciculata |
General Stability
| EC Number | General Stability | Organism |
|---|---|---|
| 1.8.1.12 | loss of 39% activity after incubation with NADPH at 25°C | Crithidia fasciculata |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.8.1.7 | Melarsen oxide | 2-step process | Homo sapiens |  |
| 1.8.1.7 | Melarsen oxide | i.e. p-(4,6-diamono-s-triazin-2-yl)aminophenylarsenoxide; potent inhibitor, reversible by excess of thiols, more sensitive with NADPH | Trypanosoma brucei gambiense | |
| 1.8.1.7 | Melarsen oxide | i.e. p-(4,6-diamono-s-triazin-2-yl)aminophenylarsenoxide; potent inhibitor, reversible by excess of thiols, more sensitive with NADPH | Trypanosoma brucei rhodesiense | |
| 1.8.1.7 | NADPH | protection by NADP+ | Homo sapiens | |
| 1.8.1.12 | arsenite | + NADPH, slightly | Crithidia fasciculata | |
| 1.8.1.12 | cymelarsen | + NADPH | Crithidia fasciculata | |
| 1.8.1.12 | Melarsen oxide | inhibition is increased in presence of NADPH, inhibition is abolished by melarsen-trypanothione disulfide adduct | Crithidia fasciculata | |
| 1.8.1.12 | melarsen-trypanothione disulfide adduct | no inhibition | Crithidia fasciculata | |
| 1.8.1.12 | melarsoprol | + NADPH, slightly | Crithidia fasciculata | |
| 1.8.1.12 | NADPH | NADPH inhibits the enzyme at higher concentration and during longer incubation times, enzyme can be protected by NADP+ | Crithidia fasciculata | |
| 1.8.1.12 | phenylarsenoxide | + NADPH | Crithidia fasciculata | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 1.8.1.7 | Bos taurus | - |
- |
- |
| 1.8.1.7 | Homo sapiens | - |
- |
- |
| 1.8.1.7 | Trypanosoma brucei gambiense | - |
parasitic protozoa | - |
| 1.8.1.7 | Trypanosoma brucei rhodesiense | - |
parasitic protozoa | - |
| 1.8.1.12 | Crithidia fasciculata | - |
- |
- |
Purification (Commentary)
| EC Number | Purification (Comment) | Organism |
|---|---|---|
| 1.8.1.7 | - |
Homo sapiens |
| 1.8.1.7 | - |
Bos taurus |
| 1.8.1.12 | - |
Crithidia fasciculata |
Reaction
| EC Number | Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|---|
| 1.8.1.7 | 2 glutathione + NADP+ = glutathione disulfide + NADPH + H+ | inhibition mechanism | Homo sapiens | |
| 1.8.1.7 | 2 glutathione + NADP+ = glutathione disulfide + NADPH + H+ | analogous to trypanothione reductase | Trypanosoma brucei rhodesiense | |
| 1.8.1.7 | 2 glutathione + NADP+ = glutathione disulfide + NADPH + H+ | analogous to trypanothione reductase | Trypanosoma brucei gambiense |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 1.8.1.7 | erythrocyte | - |
Homo sapiens | - |
| 1.8.1.7 | intestine | mucosa | Bos taurus | - |
Specific Activity [micromol/min/mg]
| EC Number | Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|---|
| 1.8.1.7 | 114 | - |
purified enzyme | Bos taurus |
| 1.8.1.7 | 262 | - |
purified enzyme | Homo sapiens |
| 1.8.1.12 | 247 | - |
purified enzyme | Crithidia fasciculata |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.8.1.7 | GSSG + NADPH | - |
Homo sapiens | glutathione + NADP+ | - |
? | |
| 1.8.1.7 | GSSG + NADPH | - |
Bos taurus | glutathione + NADP+ | - |
? | |
| 1.8.1.7 | GSSG + NADPH | - |
Trypanosoma brucei rhodesiense | glutathione + NADP+ | - |
? | |
| 1.8.1.7 | GSSG + NADPH | - |
Trypanosoma brucei gambiense | glutathione + NADP+ | - |
? | |
| 1.8.1.12 | trypanothione disulfide + NADPH | - |
Crithidia fasciculata | trypanothione + NADP+ | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 1.8.1.12 | TR | - |
Crithidia fasciculata |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 1.8.1.7 | 27 | - |
assay at | Homo sapiens |
| 1.8.1.7 | 27 | - |
assay at | Bos taurus |
| 1.8.1.7 | 27 | - |
assay at | Trypanosoma brucei rhodesiense |
| 1.8.1.7 | 27 | - |
assay at | Trypanosoma brucei gambiense |
| 1.8.1.12 | 27 | - |
assay at | Crithidia fasciculata |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 1.8.1.7 | 7.8 | - |
assay at | Homo sapiens |
| 1.8.1.7 | 7.8 | - |
assay at | Bos taurus |
| 1.8.1.12 | 7.8 | - |
assay at | Crithidia fasciculata |
Cofactor
| EC Number | Cofactor | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.8.1.7 | FAD | FAD enzyme | Homo sapiens | |
| 1.8.1.7 | FAD | FAD enzyme | Bos taurus | |
| 1.8.1.7 | FAD | FAD enzyme | Trypanosoma brucei rhodesiense | |
| 1.8.1.7 | FAD | FAD enzyme | Trypanosoma brucei gambiense | |
| 1.8.1.12 | FAD | - |
Crithidia fasciculata | |
| 1.8.1.12 | NADPH | - |
Crithidia fasciculata | |
Ki Value [mM]
| EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 1.8.1.12 | 0.016 | - |
Melarsen oxide | with melarsen-trypanothione disulfide-adduct | Crithidia fasciculata | |
| 1.8.1.12 | 0.0172 | - |
Melarsen oxide | with NADPH | Crithidia fasciculata | |
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