BRENDA - Enzyme Database show

Methylation of arsenic by recombinant human wild-type arsenic (+3 oxidation state) methyltransferase and its methionine 287 threonine (M287T) polymorph: Role of glutathione

Ding, L.; Saunders, R.J.; Drobna, Z.; Walton, F.S.; Xun, P.; Thomas, D.J.; Styblo, M.; Toxicol. Appl. Pharmacol. 264, 121-130 (2012)

Data extracted from this reference:

Activating Compound
EC Number
Activating Compound
Commentary
Organism
Structure
2.1.1.137
glutathione
1 mM GSH decreases Km and increases Vmax estimates for arsenite and methylarsonous acid
Homo sapiens
Cloned(Commentary)
EC Number
Commentary
Organism
2.1.1.137
expressed in Escherichia coli BL21(DE3)pLysS cells
Homo sapiens
Engineering
EC Number
Amino acid exchange
Commentary
Organism
2.1.1.137
M287T
in the absence of glutathione, the mutant shows decreased Vmax and Km for arsenite and increased Vmax and Km for methylarsonate compared to the wild type enzyme
Homo sapiens
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
2.1.1.137
glutathione
addition of 20 mM GSH sharply inhibits methylation
Homo sapiens
KM Value [mM]
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
2.1.1.137
0.0007
-
methylarsonate
wild type enzyme, in the presence of 1 mM glutathione, in 100 mM Tris-HCl buffer (pH 7.4), at 25°C
Homo sapiens
2.1.1.137
0.0009
-
methylarsonate
mutant enzyme M287T, in the presence of 1 mM glutathione, in 100 mM Tris-HCl buffer (pH 7.4), at 25°C
Homo sapiens
2.1.1.137
0.0015
-
methylarsonate
wild type enzyme, in 100 mM Tris-HCl buffer (pH 7.4), at 25°C
Homo sapiens
2.1.1.137
0.0016
-
arsenite
mutant enzyme M287T, in the presence of 1 mM glutathione, in 100 mM Tris-HCl buffer (pH 7.4), at 37°C; wild type enzyme, in the presence of 1 mM glutathione, in 100 mM Tris-HCl buffer (pH 7.4), at 37°C
Homo sapiens
2.1.1.137
0.002
-
arsenite
mutant enzyme M287T, in 100 mM Tris-HCl buffer (pH 7.4), at 37°C
Homo sapiens
2.1.1.137
0.003
-
methylarsonate
mutant enzyme M287T, in 100 mM Tris-HCl buffer (pH 7.4), at 25°C
Homo sapiens
2.1.1.137
0.0041
-
arsenite
wild type enzyme, in 100 mM Tris-HCl buffer (pH 7.4), at 37°C
Homo sapiens
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
2.1.1.137
Homo sapiens
-
-
-
Purification (Commentary)
EC Number
Commentary
Organism
2.1.1.137
Ni-NTA agarose column chromatography
Homo sapiens
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.1.1.137
S-adenosyl-L-methionine + arsenite
-
721075
Homo sapiens
S-adenosyl-L-homocysteine + methylarsonate + dimethylarsinous acid + dimethylarsinic acid
-
-
-
?
2.1.1.137
S-adenosyl-L-methionine + methylarsonate
-
721075
Homo sapiens
S-adenosyl-L-homocysteine + dimethylarsinous acid + dimethylarsinic acid
-
-
-
?
Activating Compound (protein specific)
EC Number
Activating Compound
Commentary
Organism
Structure
2.1.1.137
glutathione
1 mM GSH decreases Km and increases Vmax estimates for arsenite and methylarsonous acid
Homo sapiens
Cloned(Commentary) (protein specific)
EC Number
Commentary
Organism
2.1.1.137
expressed in Escherichia coli BL21(DE3)pLysS cells
Homo sapiens
Engineering (protein specific)
EC Number
Amino acid exchange
Commentary
Organism
2.1.1.137
M287T
in the absence of glutathione, the mutant shows decreased Vmax and Km for arsenite and increased Vmax and Km for methylarsonate compared to the wild type enzyme
Homo sapiens
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
2.1.1.137
glutathione
addition of 20 mM GSH sharply inhibits methylation
Homo sapiens
KM Value [mM] (protein specific)
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
2.1.1.137
0.0007
-
methylarsonate
wild type enzyme, in the presence of 1 mM glutathione, in 100 mM Tris-HCl buffer (pH 7.4), at 25°C
Homo sapiens
2.1.1.137
0.0009
-
methylarsonate
mutant enzyme M287T, in the presence of 1 mM glutathione, in 100 mM Tris-HCl buffer (pH 7.4), at 25°C
Homo sapiens
2.1.1.137
0.0015
-
methylarsonate
wild type enzyme, in 100 mM Tris-HCl buffer (pH 7.4), at 25°C
Homo sapiens
2.1.1.137
0.0016
-
arsenite
mutant enzyme M287T, in the presence of 1 mM glutathione, in 100 mM Tris-HCl buffer (pH 7.4), at 37°C; wild type enzyme, in the presence of 1 mM glutathione, in 100 mM Tris-HCl buffer (pH 7.4), at 37°C
Homo sapiens
2.1.1.137
0.002
-
arsenite
mutant enzyme M287T, in 100 mM Tris-HCl buffer (pH 7.4), at 37°C
Homo sapiens
2.1.1.137
0.003
-
methylarsonate
mutant enzyme M287T, in 100 mM Tris-HCl buffer (pH 7.4), at 25°C
Homo sapiens
2.1.1.137
0.0041
-
arsenite
wild type enzyme, in 100 mM Tris-HCl buffer (pH 7.4), at 37°C
Homo sapiens
Purification (Commentary) (protein specific)
EC Number
Commentary
Organism
2.1.1.137
Ni-NTA agarose column chromatography
Homo sapiens
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.1.1.137
S-adenosyl-L-methionine + arsenite
-
721075
Homo sapiens
S-adenosyl-L-homocysteine + methylarsonate + dimethylarsinous acid + dimethylarsinic acid
-
-
-
?
2.1.1.137
S-adenosyl-L-methionine + methylarsonate
-
721075
Homo sapiens
S-adenosyl-L-homocysteine + dimethylarsinous acid + dimethylarsinic acid
-
-
-
?
General Information
EC Number
General Information
Commentary
Organism
2.1.1.137
metabolism
key enzyme in the pathway for methylation of arsenicals
Homo sapiens
General Information (protein specific)
EC Number
General Information
Commentary
Organism
2.1.1.137
metabolism
key enzyme in the pathway for methylation of arsenicals
Homo sapiens