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Literature summary extracted from
- The aza-analogues of 1,4-naphthoquinones are potent substrates and inhibitors of plasmodial thioredoxin and glutathione reductases and of human erythrocyte glutathione reductase (2008), Org. Biomol. Chem., 6, 2731-2742.
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.8.1.7 | 1,4-Naphthoquinone | inhibitits activity with GSSG | Homo sapiens |  |
| 1.8.1.7 | 1,4-Naphthoquinone | inhibitits activity with GSSG | Plasmodium falciparum | |
| 1.8.1.7 | 2,3-dimethylquinoxaline-5,8-dione | inhibitits activity with GSSG | Homo sapiens | |
| 1.8.1.7 | 2,3-dimethylquinoxaline-5,8-dione | inhibitits activity with GSSG | Plasmodium falciparum | |
| 1.8.1.7 | 6,7-dimethylquinoline-5,8-dione | inhibitits activity with GSSG | Homo sapiens | |
| 1.8.1.7 | 6,7-dimethylquinoline-5,8-dione | inhibitits activity with GSSG | Plasmodium falciparum | |
| 1.8.1.7 | 6-methylquinoline-5,8-dione | inhibitits activity with GSSG | Homo sapiens | |
| 1.8.1.7 | 6-methylquinoline-5,8-dione | inhibitits activity with GSSG | Plasmodium falciparum | |
| 1.8.1.7 | 7-methylquinoline-5,8-dione | inhibitits activity with GSSG | Homo sapiens | |
| 1.8.1.7 | 7-methylquinoline-5,8-dione | inhibitits activity with GSSG | Plasmodium falciparum | |
| 1.8.1.7 | menadione | inhibitits activity with GSSG | Homo sapiens | |
| 1.8.1.7 | menadione | inhibitits activity with GSSG | Plasmodium falciparum | |
| 1.8.1.7 | additional information | IC50 for quinoline-5,8-dione is above 0.15 mM | Homo sapiens | |
| 1.8.1.7 | additional information | IC50 for quinoline-5,8-dione is above 0.13 mM | Plasmodium falciparum | |
| 1.8.1.7 | quinoxaline-5,8-dione | inhibitits activity with GSSG | Homo sapiens | |
| 1.8.1.7 | quinoxaline-5,8-dione | inhibitits activity with GSSG | Plasmodium falciparum | |
KM Value [mM]
| EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 1.8.1.7 | 0.0312 | - |
menadione | 25°C | Homo sapiens | |
| 1.8.1.7 | 0.0562 | - |
quinoxaline-5,8-dione | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 0.0595 | - |
quinoxaline-5,8-dione | 25°C | Homo sapiens | |
| 1.8.1.7 | 0.0822 | - |
menadione | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 0.0858 | - |
6,7-dimethylquinoline-5,8-dione | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 0.158 | - |
1,4-Naphthoquinone | 25°C | Homo sapiens | |
| 1.8.1.7 | 0.172 | - |
1,4-Naphthoquinone | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 0.224 | - |
7-methylquinoline-5,8-dione | 25°C | Homo sapiens | |
| 1.8.1.7 | 0.234 | - |
quinoline-5,8-dione | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 0.363 | - |
quinoline-5,8-dione | 25°C | Homo sapiens | |
| 1.8.1.7 | 0.404 | - |
7-methylquinoline-5,8-dione | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 0.4104 | - |
6-methylquinoline-5,8-dione | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 0.413 | - |
6,7-dimethylquinoline-5,8-dione | 25°C | Homo sapiens | |
| 1.8.1.7 | 0.4208 | - |
6-methylquinoline-5,8-dione | 25°C | Homo sapiens | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 1.8.1.7 | Homo sapiens | - |
- |
- |
| 1.8.1.7 | Plasmodium falciparum | - |
- |
- |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.8.1.7 | 1,4-naphthoquinone + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| 1.8.1.7 | 1,4-naphthoquinone + NADPH + H+ | - |
Plasmodium falciparum | ? | - |
? | |
| 1.8.1.7 | 2,3-dimethylquinoxaline-5,8-dione + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| 1.8.1.7 | 2,3-dimethylquinoxaline-5,8-dione + NADPH + H+ | - |
Plasmodium falciparum | ? | - |
? | |
| 1.8.1.7 | 6,7-dimethylquinoline-5,8-dione + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| 1.8.1.7 | 6,7-dimethylquinoline-5,8-dione + NADPH + H+ | - |
Plasmodium falciparum | ? | - |
? | |
| 1.8.1.7 | 6-methylquinoline-5,8-dione + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| 1.8.1.7 | 6-methylquinoline-5,8-dione + NADPH + H+ | - |
Plasmodium falciparum | ? | - |
? | |
| 1.8.1.7 | 7-methylquinoline-5,8-dione + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| 1.8.1.7 | 7-methylquinoline-5,8-dione + NADPH + H+ | - |
Plasmodium falciparum | ? | - |
? | |
| 1.8.1.7 | GSSG + NADPH + H+ | - |
Homo sapiens | glutathione + NADP+ | - |
? | |
| 1.8.1.7 | GSSG + NADPH + H+ | - |
Plasmodium falciparum | glutathione + NADP+ | - |
? | |
| 1.8.1.7 | menadione + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| 1.8.1.7 | menadione + NADPH + H+ | - |
Plasmodium falciparum | ? | - |
? | |
| 1.8.1.7 | quinoline-5,8-dione + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| 1.8.1.7 | quinoline-5,8-dione + NADPH + H+ | - |
Plasmodium falciparum | ? | - |
? | |
| 1.8.1.7 | quinoxaline-5,8-dione + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| 1.8.1.7 | quinoxaline-5,8-dione + NADPH + H+ | - |
Plasmodium falciparum | ? | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 1.8.1.7 | hGR | - |
Homo sapiens |
| 1.8.1.7 | PfGR | - |
Plasmodium falciparum |
Turnover Number [1/s]
| EC Number | Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 1.8.1.7 | 0.08 | - |
6,7-dimethylquinoline-5,8-dione | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 0.11 | - |
6,7-dimethylquinoline-5,8-dione | 25°C | Homo sapiens | |
| 1.8.1.7 | 0.13 | - |
7-methylquinoline-5,8-dione | 25°C | Homo sapiens | |
| 1.8.1.7 | 0.16 | - |
menadione | 25°C | Homo sapiens | |
| 1.8.1.7 | 0.16 | - |
menadione | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 0.34 | - |
quinoxaline-5,8-dione | 25°C | Homo sapiens | |
| 1.8.1.7 | 0.35 | - |
6-methylquinoline-5,8-dione | 25°C | Homo sapiens | |
| 1.8.1.7 | 0.35 | - |
6-methylquinoline-5,8-dione | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 0.35 | - |
quinoxaline-5,8-dione | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 0.39 | - |
7-methylquinoline-5,8-dione | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 1.08 | - |
1,4-Naphthoquinone | 25°C | Homo sapiens | |
| 1.8.1.7 | 1.08 | - |
1,4-Naphthoquinone | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 1.55 | - |
quinoline-5,8-dione | 25°C | Plasmodium falciparum | |
| 1.8.1.7 | 2.23 | - |
quinoline-5,8-dione | 25°C | Homo sapiens | |
Cofactor
| EC Number | Cofactor | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.8.1.7 | NADPH | - |
Homo sapiens | |
| 1.8.1.7 | NADPH | - |
Plasmodium falciparum | |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 1.8.1.7 | 0.0013 | - |
25°C | Homo sapiens | 1,4-Naphthoquinone | |
| 1.8.1.7 | 0.0022 | - |
25°C | Plasmodium falciparum | 1,4-Naphthoquinone | |
| 1.8.1.7 | 0.009 | - |
25°C | Homo sapiens | 6-methylquinoline-5,8-dione | |
| 1.8.1.7 | 0.011 | - |
25°C | Plasmodium falciparum | 6-methylquinoline-5,8-dione | |
| 1.8.1.7 | 0.013 | - |
25°C | Homo sapiens | 7-methylquinoline-5,8-dione | |
| 1.8.1.7 | 0.018 | - |
25°C | Homo sapiens | 6,7-dimethylquinoline-5,8-dione | |
| 1.8.1.7 | 0.025 | - |
25°C | Plasmodium falciparum | 6,7-dimethylquinoline-5,8-dione | |
| 1.8.1.7 | 0.028 | - |
25°C | Plasmodium falciparum | 7-methylquinoline-5,8-dione | |
| 1.8.1.7 | 0.034 | - |
25°C | Homo sapiens | 2,3-dimethylquinoxaline-5,8-dione | |
| 1.8.1.7 | 0.036 | - |
25°C | Homo sapiens | quinoxaline-5,8-dione | |
| 1.8.1.7 | 0.037 | - |
25°C | Plasmodium falciparum | quinoxaline-5,8-dione | |
| 1.8.1.7 | 0.085 | - |
25°C | Plasmodium falciparum | 2,3-dimethylquinoxaline-5,8-dione | |
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