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Literature summary for 1.8.1.7 extracted from

  • Morin, C.; Besset, T.; Moutet, J.C.; Fayolle, M.; Brueckner, M.; Limosin, D.; Becker, K.; Davioud-Charvet, E.
    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.
    View publication on PubMed
Search for more literature for 1.8.1.7

Inhibitors

Inhibitors Comment Organism Structure
1,4-Naphthoquinone inhibitits activity with GSSG Homo sapiens
1,4-Naphthoquinone inhibitits activity with GSSG Plasmodium falciparum
2,3-dimethylquinoxaline-5,8-dione inhibitits activity with GSSG Homo sapiens
2,3-dimethylquinoxaline-5,8-dione inhibitits activity with GSSG Plasmodium falciparum
6,7-dimethylquinoline-5,8-dione inhibitits activity with GSSG Homo sapiens
6,7-dimethylquinoline-5,8-dione inhibitits activity with GSSG Plasmodium falciparum
6-methylquinoline-5,8-dione inhibitits activity with GSSG Homo sapiens
6-methylquinoline-5,8-dione inhibitits activity with GSSG Plasmodium falciparum
7-methylquinoline-5,8-dione inhibitits activity with GSSG Homo sapiens
7-methylquinoline-5,8-dione inhibitits activity with GSSG Plasmodium falciparum
menadione inhibitits activity with GSSG Homo sapiens
menadione inhibitits activity with GSSG Plasmodium falciparum
additional information IC50 for quinoline-5,8-dione is above 0.15 mM Homo sapiens
additional information IC50 for quinoline-5,8-dione is above 0.13 mM Plasmodium falciparum
quinoxaline-5,8-dione inhibitits activity with GSSG Homo sapiens
quinoxaline-5,8-dione inhibitits activity with GSSG Plasmodium falciparum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0312
-
 menadione 25°C Homo sapiens
0.0562
-
 quinoxaline-5,8-dione 25°C Plasmodium falciparum
0.0595
-
 quinoxaline-5,8-dione 25°C Homo sapiens
0.0822
-
 menadione 25°C Plasmodium falciparum
0.0858
-
 6,7-dimethylquinoline-5,8-dione 25°C Plasmodium falciparum
0.158
-
 1,4-Naphthoquinone 25°C Homo sapiens
0.172
-
 1,4-Naphthoquinone 25°C Plasmodium falciparum
0.224
-
 7-methylquinoline-5,8-dione 25°C Homo sapiens
0.234
-
 quinoline-5,8-dione 25°C Plasmodium falciparum
0.363
-
 quinoline-5,8-dione 25°C Homo sapiens
0.404
-
 7-methylquinoline-5,8-dione 25°C Plasmodium falciparum
0.4104
-
 6-methylquinoline-5,8-dione 25°C Plasmodium falciparum
0.413
-
 6,7-dimethylquinoline-5,8-dione 25°C Homo sapiens
0.4208
-
 6-methylquinoline-5,8-dione 25°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Plasmodium falciparum
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1,4-naphthoquinone + NADPH + H+
-
 Homo sapiens ?
-
 ?
1,4-naphthoquinone + NADPH + H+
-
 Plasmodium falciparum ?
-
 ?
2,3-dimethylquinoxaline-5,8-dione + NADPH + H+
-
 Homo sapiens ?
-
 ?
2,3-dimethylquinoxaline-5,8-dione + NADPH + H+
-
 Plasmodium falciparum ?
-
 ?
6,7-dimethylquinoline-5,8-dione + NADPH + H+
-
 Homo sapiens ?
-
 ?
6,7-dimethylquinoline-5,8-dione + NADPH + H+
-
 Plasmodium falciparum ?
-
 ?
6-methylquinoline-5,8-dione + NADPH + H+
-
 Homo sapiens ?
-
 ?
6-methylquinoline-5,8-dione + NADPH + H+
-
 Plasmodium falciparum ?
-
 ?
7-methylquinoline-5,8-dione + NADPH + H+
-
 Homo sapiens ?
-
 ?
7-methylquinoline-5,8-dione + NADPH + H+
-
 Plasmodium falciparum ?
-
 ?
GSSG + NADPH + H+
-
 Homo sapiens glutathione + NADP+
-
 ?
GSSG + NADPH + H+
-
 Plasmodium falciparum glutathione + NADP+
-
 ?
menadione + NADPH + H+
-
 Homo sapiens ?
-
 ?
menadione + NADPH + H+
-
 Plasmodium falciparum ?
-
 ?
quinoline-5,8-dione + NADPH + H+
-
 Homo sapiens ?
-
 ?
quinoline-5,8-dione + NADPH + H+
-
 Plasmodium falciparum ?
-
 ?
quinoxaline-5,8-dione + NADPH + H+
-
 Homo sapiens ?
-
 ?
quinoxaline-5,8-dione + NADPH + H+
-
 Plasmodium falciparum ?
-
 ?

Synonyms

Synonyms Comment Organism
hGR
-
 Homo sapiens
PfGR
-
 Plasmodium falciparum

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.08
-
 6,7-dimethylquinoline-5,8-dione 25°C Plasmodium falciparum
0.11
-
 6,7-dimethylquinoline-5,8-dione 25°C Homo sapiens
0.13
-
 7-methylquinoline-5,8-dione 25°C Homo sapiens
0.16
-
 menadione 25°C Homo sapiens
0.16
-
 menadione 25°C Plasmodium falciparum
0.34
-
 quinoxaline-5,8-dione 25°C Homo sapiens
0.35
-
 6-methylquinoline-5,8-dione 25°C Homo sapiens
0.35
-
 6-methylquinoline-5,8-dione 25°C Plasmodium falciparum
0.35
-
 quinoxaline-5,8-dione 25°C Plasmodium falciparum
0.39
-
 7-methylquinoline-5,8-dione 25°C Plasmodium falciparum
1.08
-
 1,4-Naphthoquinone 25°C Homo sapiens
1.08
-
 1,4-Naphthoquinone 25°C Plasmodium falciparum
1.55
-
 quinoline-5,8-dione 25°C Plasmodium falciparum
2.23
-
 quinoline-5,8-dione 25°C Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
 Homo sapiens
NADPH
-
 Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0013
-
 25°C Homo sapiens 1,4-Naphthoquinone
0.0022
-
 25°C Plasmodium falciparum 1,4-Naphthoquinone
0.009
-
 25°C Homo sapiens 6-methylquinoline-5,8-dione
0.011
-
 25°C Plasmodium falciparum 6-methylquinoline-5,8-dione
0.013
-
 25°C Homo sapiens 7-methylquinoline-5,8-dione
0.018
-
 25°C Homo sapiens 6,7-dimethylquinoline-5,8-dione
0.025
-
 25°C Plasmodium falciparum 6,7-dimethylquinoline-5,8-dione
0.028
-
 25°C Plasmodium falciparum 7-methylquinoline-5,8-dione
0.034
-
 25°C Homo sapiens 2,3-dimethylquinoxaline-5,8-dione
0.036
-
 25°C Homo sapiens quinoxaline-5,8-dione
0.037
-
 25°C Plasmodium falciparum quinoxaline-5,8-dione
0.085
-
 25°C Plasmodium falciparum 2,3-dimethylquinoxaline-5,8-dione