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Literature summary for 3.1.1.7 extracted from

  • Kovarik, Z.; Ciban, N.; Radic, Z.; Simeon-Rudolf, V.; Taylor, P.
    Active site mutant acetylcholinesterase interactions with 2-PAM, HI-6, and DDVP (2006), Biochem. Biophys. Res. Commun., 342, 973-978.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
F295L analysis of inhibition kinetics for 2-((Z)-(hydroxyimino)methyl)-1-methylpyridinium chloride, 4-(aminocarbonyl)-1-(((2-((Z)-(hydroxyimino)methyl)pyridinium-1-yl)methoxy)methyl)pyridinium dichloride, and 2,2-dichlorovinyl dimethyl phosphate Mus musculus
F297I analysis of inhibition kinetics for 2-((Z)-(hydroxyimino)methyl)-1-methylpyridinium chloride, 4-(aminocarbonyl)-1-(((2-((Z)-(hydroxyimino)methyl)pyridinium-1-yl)methoxy)methyl)pyridinium dichloride, and 2,2-dichlorovinyl dimethyl phosphate Mus musculus
W286A analysis of inhibition kinetics for 2-((Z)-(hydroxyimino)methyl)-1-methylpyridinium chloride, 4-(aminocarbonyl)-1-(((2-((Z)-(hydroxyimino)methyl)pyridinium-1-yl)methoxy)methyl)pyridinium dichloride, and 2,2-dichlorovinyl dimethyl phosphate Mus musculus
Y124Q analysis of inhibition kinetics for 2-((Z)-(hydroxyimino)methyl)-1-methylpyridinium chloride, 4-(aminocarbonyl)-1-(((2-((Z)-(hydroxyimino)methyl)pyridinium-1-yl)methoxy)methyl)pyridinium dichloride, and 2,2-dichlorovinyl dimethyl phosphate Mus musculus
Y337A analysis of inhibition kinetics for 2-((Z)-(hydroxyimino)methyl)-1-methylpyridinium chloride, 4-(aminocarbonyl)-1-(((2-((Z)-(hydroxyimino)methyl)pyridinium-1-yl)methoxy)methyl)pyridinium dichloride, and 2,2-dichlorovinyl dimethyl phosphate Mus musculus
Y72N analysis of inhibition kinetics for 2-((Z)-(hydroxyimino)methyl)-1-methylpyridinium chloride, 4-(aminocarbonyl)-1-(((2-((Z)-(hydroxyimino)methyl)pyridinium-1-yl)methoxy)methyl)pyridinium dichloride, and 2,2-dichlorovinyl dimethyl phosphate Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
2,2-dichlorovinyl dimethyl phosphate i.e. DDVP, reversible, detailed kinetic analysis Mus musculus
2-((Z)-(hydroxyimino)methyl)-1-methylpyridinium chloride i.e. 2-PAM, reversible, detailed kinetic analysis Mus musculus
4-(aminocarbonyl)-1-(((2-((Z)-(hydroxyimino)methyl)pyridinium-1-yl)methoxy)methyl)pyridinium dichloride i.e. HI-6, reversible, detailed kinetic analysis Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
-
recombinant enzyme
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.046
-
4-(aminocarbonyl)-1-(((2-((Z)-(hydroxyimino)methyl)pyridinium-1-yl)methoxy)methyl)pyridinium dichloride pH 7.0, 25°C, wild-type Mus musculus
0.087
-
4-(aminocarbonyl)-1-(((2-((Z)-(hydroxyimino)methyl)pyridinium-1-yl)methoxy)methyl)pyridinium dichloride pH 7.0, 25°C, mutant Y337A Mus musculus
0.11
-
4-(aminocarbonyl)-1-(((2-((Z)-(hydroxyimino)methyl)pyridinium-1-yl)methoxy)methyl)pyridinium dichloride pH 7.0, 25°C, mutant F295L/Y337A Mus musculus
0.15
-
2-((Z)-(hydroxyimino)methyl)-1-methylpyridinium chloride pH 7.0, 25°C, wild-type Mus musculus
0.18
-
4-(aminocarbonyl)-1-(((2-((Z)-(hydroxyimino)methyl)pyridinium-1-yl)methoxy)methyl)pyridinium dichloride pH 7.0, 25°C, mutant F297I/Y337A Mus musculus
0.28
-
2-((Z)-(hydroxyimino)methyl)-1-methylpyridinium chloride pH 7.0, 25°C, mutant Y72N/Y124Q/W286A Mus musculus
0.36
-
4-(aminocarbonyl)-1-(((2-((Z)-(hydroxyimino)methyl)pyridinium-1-yl)methoxy)methyl)pyridinium dichloride pH 7.0, 25°C, mutant Y72N/Y124Q/W286A Mus musculus
0.59
-
2-((Z)-(hydroxyimino)methyl)-1-methylpyridinium chloride pH 7.0, 25°C, mutant Y337A Mus musculus
0.65
-
2-((Z)-(hydroxyimino)methyl)-1-methylpyridinium chloride pH 7.0, 25°C, mutant F295L/Y337A Mus musculus
1.7
-
2-((Z)-(hydroxyimino)methyl)-1-methylpyridinium chloride pH 7.0, 25°C, mutant F297I/Y337A Mus musculus