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Literature summary extracted from

  • Bauer, H.; Fritz-Wolf, K.; Winzer, A.; Kuehner, S.; Little, S.; Yardley, V.; Vezin, H.; Palfey, B.; Schirmer, R.H.; Davioud-Charvet, E.
    A fluoro analogue of the menadione derivative 6-[2-(3-methyl)-1,4-naphthoquinolyl]hexanoic acid is a suicide substrate of glutathione reductase. Crystal structure of the alkylated human enzyme (2006), J. Am. Chem. Soc., 128, 10784-10794.
    View publication on PubMed

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.8.1.7 hanging drop vapour diffusion method Homo sapiens
1.8.1.7 hanging drop vapour diffusion method Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.8.1.7 6-[2-(3-fluoromethyl)-1,4-naphthoquinolyl]hexanoic acid IC50: 0.0041 mM, irreversible inhibition Homo sapiens
1.8.1.7 6-[2-(3-fluoromethyl)-1,4-naphthoquinolyl]hexanoic acid IC50: 0.0064 mM, at pH 6.9 and 25°C in the presence of 1 mM GSSG, irreversible inhibition Plasmodium falciparum
1.8.1.7 6-[2-(3-methyl)-1,4-naphthoquinolyl]hexanoic acid IC50: 0.0032 mM, uncompetitive inhibitor Homo sapiens
1.8.1.7 6-[2-(3-methyl)-1,4-naphthoquinolyl]hexanoic acid IC50: 0.0045 mM, at pH 6.9 and 25°C in the presence of 1 mM GSSG, uncompetitive inhibitor Plasmodium falciparum
1.8.1.7 menadione IC50: 0.0275 mM Homo sapiens
1.8.1.7 menadione IC50: 0.042 mM, at pH 6.9 and 25°C in the presence of 1 mM GSSG Plasmodium falciparum
1.8.1.7 [4-(3-methyl-1,4-dioxo-1,2,3,4-tetrahydronaphthalen-2-yl)phenyl]acetic acid IC50: 0.0014 mM Homo sapiens
1.8.1.7 [4-(3-methyl-1,4-dioxo-1,2,3,4-tetrahydronaphthalen-2-yl)phenyl]acetic acid IC50: 0.0077 mM, at pH 6.9 and 25°C in the presence of 1 mM GSSG Plasmodium falciparum
1.8.1.7 [4-[3-(fluoromethyl)-1,4-dioxo-1,2,3,4-tetrahydronaphthalen-2-yl]phenyl]acetic acid IC50: 0.0035 mM Homo sapiens
1.8.1.7 [4-[3-(fluoromethyl)-1,4-dioxo-1,2,3,4-tetrahydronaphthalen-2-yl]phenyl]acetic acid IC50: 0.002 mM, at pH 6.9 and 25°C in the presence of 1 mM GSSG Plasmodium falciparum

Organism

EC Number Organism UniProt Comment Textmining
1.8.1.7 Homo sapiens
-
-
-
1.8.1.7 Plasmodium falciparum
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.8.1.7 glutathione disulfide + NADPH + H+
-
 Homo sapiens glutathione + NADP+
-
 ?
1.8.1.7 glutathione disulfide + NADPH + H+
-
 Plasmodium falciparum glutathione + NADP+
-
 ?

Subunits

EC Number Subunits Comment Organism
1.8.1.7 homodimer
-
 Homo sapiens
1.8.1.7 homodimer
-
 Plasmodium falciparum

Synonyms

EC Number Synonyms Comment Organism
1.8.1.7 glutathione reductase
-
 Homo sapiens
1.8.1.7 glutathione reductase
-
 Plasmodium falciparum
1.8.1.7 GR
-
 Homo sapiens
1.8.1.7 GR
-
 Plasmodium falciparum

Cofactor

EC Number Cofactor Comment Organism Structure
1.8.1.7 FAD
-
 Homo sapiens
1.8.1.7 FAD
-
 Plasmodium falciparum

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.8.1.7 0.0014
-
 IC50: 0.0014 mM Homo sapiens [4-(3-methyl-1,4-dioxo-1,2,3,4-tetrahydronaphthalen-2-yl)phenyl]acetic acid
1.8.1.7 0.002
-
 IC50: 0.002 mM, at pH 6.9 and 25°C in the presence of 1 mM GSSG Plasmodium falciparum [4-[3-(fluoromethyl)-1,4-dioxo-1,2,3,4-tetrahydronaphthalen-2-yl]phenyl]acetic acid
1.8.1.7 0.0032
-
 IC50: 0.0032 mM, uncompetitive inhibitor Homo sapiens 6-[2-(3-methyl)-1,4-naphthoquinolyl]hexanoic acid
1.8.1.7 0.0035
-
 IC50: 0.0035 mM Homo sapiens [4-[3-(fluoromethyl)-1,4-dioxo-1,2,3,4-tetrahydronaphthalen-2-yl]phenyl]acetic acid
1.8.1.7 0.0041
-
 IC50: 0.0041 mM, irreversible inhibition Homo sapiens 6-[2-(3-fluoromethyl)-1,4-naphthoquinolyl]hexanoic acid
1.8.1.7 0.0045
-
 IC50: 0.0045 mM, at pH 6.9 and 25°C in the presence of 1 mM GSSG, uncompetitive inhibitor Plasmodium falciparum 6-[2-(3-methyl)-1,4-naphthoquinolyl]hexanoic acid
1.8.1.7 0.0064
-
 IC50: 0.0064 mM, at pH 6.9 and 25°C in the presence of 1 mM GSSG, irreversible inhibition Plasmodium falciparum 6-[2-(3-fluoromethyl)-1,4-naphthoquinolyl]hexanoic acid
1.8.1.7 0.0077
-
 IC50: 0.0077 mM, at pH 6.9 and 25°C in the presence of 1 mM GSSG Plasmodium falciparum [4-(3-methyl-1,4-dioxo-1,2,3,4-tetrahydronaphthalen-2-yl)phenyl]acetic acid
1.8.1.7 0.0275
-
 IC50: 0.0275 mM Homo sapiens menadione
1.8.1.7 0.042
-
 IC50: 0.042 mM, at pH 6.9 and 25°C in the presence of 1 mM GSSG Plasmodium falciparum menadione