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Literature summary extracted from
- Inhibition of Trypanosoma cruzi trypanothione reductase by acridines: kinetic studies and structure-activity relationships (1999), J. Med. Chem., 42, 5448-5454.
Activating Compound
| EC Number | Activating Compound | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.8.1.12 | additional information | activity is dependent on a redox-active cysteine at the active centre | Trypanosoma cruzi |
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 1.8.1.12 | medicine | potential target for drug design against trypanosomiasis | Trypanosoma cruzi |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.8.1.12 | 6-chlorotacrine | competitive inhibition | Trypanosoma cruzi |  |
| 1.8.1.12 | 9-Amino-1,2,3,4-tetrahydroacridine | i.e. tacrine, competitive inhibition | Trypanosoma cruzi | |
| 1.8.1.12 | 9-aminoacridine derivatives | competitive inhibition | Trypanosoma cruzi | |
| 1.8.1.12 | 9-thioacridine derivatives | mixed-type inhibition | Trypanosoma cruzi | |
| 1.8.1.12 | Mepacrine | i.e. quinacrine, competitive inhibition | Trypanosoma cruzi | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 1.8.1.12 | Trypanosoma cruzi | - |
- |
- |
Reaction
| EC Number | Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|---|
| 1.8.1.12 | trypanothione + NADP+ = trypanothione disulfide + NADPH + H+ | mechanistic reaction scheme, structure-function relation | Trypanosoma cruzi |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.8.1.12 | trypanothione disulfide + NADPH | - |
Trypanosoma cruzi | trypanothione + NADP+ | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 1.8.1.12 | TR | - |
Trypanosoma cruzi |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 1.8.1.12 | 25 | - |
assay at | Trypanosoma cruzi |
Cofactor
| EC Number | Cofactor | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.8.1.12 | FAD | - |
Trypanosoma cruzi | |
| 1.8.1.12 | NADPH | - |
Trypanosoma cruzi | |
Ki Value [mM]
| EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 1.8.1.12 | 0.007 | 0.043 | 9-aminoacridine derivatives | - |
Trypanosoma cruzi | |
| 1.8.1.12 | 0.019 | - |
Mepacrine | - |
Trypanosoma cruzi | |
| 1.8.1.12 | 0.021 | 0.037 | 9-thioacridine derivatives | - |
Trypanosoma cruzi | |
| 1.8.1.12 | 0.08 | - |
6-chlorotacrine | - |
Trypanosoma cruzi | |
| 1.8.1.12 | 0.14 | - |
9-Amino-1,2,3,4-tetrahydroacridine | - |
Trypanosoma cruzi | |
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Release 2023.1 (January 2023)
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