BRENDA - Enzyme Database

Structural characterization, biochemical, inhibition and computational studies of Entamoeba histolytica phosphoglycerate mutase finding hits for a new antiamoebic drug

la Cruz, A.; Sanabria-Chanaga, E.; Yepez-Mulia, L.; Castillo, R.; Hernandez-Campos, A.; Najera, H.; Avitia-Dominguez, C.; Sierra-Campos, E.; Valdez-Solana, M.; Tellez-Valencia, A.; Med. Chem. Res. 27, 1705-1716 (2018)
No PubMed abstract available

Data extracted from this reference:

Cloned(Commentary)
EC Number
Commentary
Organism
5.4.2.12
expressed in Escherichia coli BLR(DE3) cells
Entamoeba histolytica
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
5.4.2.12
1-methyl-2-(methylthio)-1H-benzimidazole-5-carboxamide
54% inhibition at 0.1 mM
Entamoeba histolytica
5.4.2.12
1-methyl-2-(methylthio)-N-(5-nitro-1,3-thiazol-2-yl)-1H-benzimidazole-6-carboxamide
47% inhibition at 0.1 mM
Entamoeba histolytica
5.4.2.12
1H-benzimidazole-5-carboxylic acid
69% inhibition at 0.1 mM
Entamoeba histolytica
5.4.2.12
2-(4-nitrophenyl)-1H-benzimidazole-7-carboxylic acid
56% inhibition at 0.1 mM
Entamoeba histolytica
5.4.2.12
6-chloro-2-(4-nitrophenyl)-1H-benzimidazole-7-carboxylic acid
59% inhibition at 0.1 mM
Entamoeba histolytica
5.4.2.12
6-chloro-2-(methylthio)-1H-benzimidazole-5-carboxylic acid
73% inhibition at 0.1 mM
Entamoeba histolytica
5.4.2.12
6-chloro-2-(methylthio)-N-(5-nitro-1,3-thiazol-2-yl)-1H-benzimidazole-5-carboxamide
47% inhibition at 0.1 mM
Entamoeba histolytica
KM Value [mM]
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
5.4.2.12
0.773
-
3-phospho-D-glycerate
at pH 6.0 and 37°C
Entamoeba histolytica
Molecular Weight [Da]
EC Number
Molecular Weight [Da]
Molecular Weight Maximum [Da]
Commentary
Organism
5.4.2.12
57000
-
gel filtration
Entamoeba histolytica
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
5.4.2.12
2-phospho-D-glycerate
Entamoeba histolytica
-
3-phospho-D-glycerate
-
-
r
5.4.2.12
2-phospho-D-glycerate
Entamoeba histolytica HM1 IMSS
-
3-phospho-D-glycerate
-
-
r
5.4.2.12
3-phospho-D-glycerate
Entamoeba histolytica
-
2-phospho-D-glycerate
-
-
r
5.4.2.12
3-phospho-D-glycerate
Entamoeba histolytica HM1 IMSS
-
2-phospho-D-glycerate
-
-
r
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
5.4.2.12
Entamoeba histolytica
C4LTW4
-
-
5.4.2.12
Entamoeba histolytica HM1 IMSS
C4LTW4
-
-
Purification (Commentary)
EC Number
Commentary
Organism
5.4.2.12
Ni-NTA column chromatography
Entamoeba histolytica
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
5.4.2.12
2-phospho-D-glycerate
-
748541
Entamoeba histolytica
3-phospho-D-glycerate
-
-
-
r
5.4.2.12
2-phospho-D-glycerate
-
748541
Entamoeba histolytica HM1 IMSS
3-phospho-D-glycerate
-
-
-
r
5.4.2.12
3-phospho-D-glycerate
-
748541
Entamoeba histolytica
2-phospho-D-glycerate
-
-
-
r
5.4.2.12
3-phospho-D-glycerate
-
748541
Entamoeba histolytica HM1 IMSS
2-phospho-D-glycerate
-
-
-
r
Subunits
EC Number
Subunits
Commentary
Organism
5.4.2.12
monomer
1 * 64000, SDS-PAGE
Entamoeba histolytica
Cofactor
EC Number
Cofactor
Commentary
Organism
Structure
5.4.2.12
additional information
the enzyme is independent from 2,3-bisphosphoglycerate
Entamoeba histolytica
Cloned(Commentary) (protein specific)
EC Number
Commentary
Organism
5.4.2.12
expressed in Escherichia coli BLR(DE3) cells
Entamoeba histolytica
Cofactor (protein specific)
EC Number
Cofactor
Commentary
Organism
Structure
5.4.2.12
additional information
the enzyme is independent from 2,3-bisphosphoglycerate
Entamoeba histolytica
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
5.4.2.12
1-methyl-2-(methylthio)-1H-benzimidazole-5-carboxamide
54% inhibition at 0.1 mM
Entamoeba histolytica
5.4.2.12
1-methyl-2-(methylthio)-N-(5-nitro-1,3-thiazol-2-yl)-1H-benzimidazole-6-carboxamide
47% inhibition at 0.1 mM
Entamoeba histolytica
5.4.2.12
1H-benzimidazole-5-carboxylic acid
69% inhibition at 0.1 mM
Entamoeba histolytica
5.4.2.12
2-(4-nitrophenyl)-1H-benzimidazole-7-carboxylic acid
56% inhibition at 0.1 mM
Entamoeba histolytica
5.4.2.12
6-chloro-2-(4-nitrophenyl)-1H-benzimidazole-7-carboxylic acid
59% inhibition at 0.1 mM
Entamoeba histolytica
5.4.2.12
6-chloro-2-(methylthio)-1H-benzimidazole-5-carboxylic acid
73% inhibition at 0.1 mM
Entamoeba histolytica
5.4.2.12
6-chloro-2-(methylthio)-N-(5-nitro-1,3-thiazol-2-yl)-1H-benzimidazole-5-carboxamide
47% inhibition at 0.1 mM
Entamoeba histolytica
KM Value [mM] (protein specific)
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
5.4.2.12
0.773
-
3-phospho-D-glycerate
at pH 6.0 and 37°C
Entamoeba histolytica
Molecular Weight [Da] (protein specific)
EC Number
Molecular Weight [Da]
Molecular Weight Maximum [Da]
Commentary
Organism
5.4.2.12
57000
-
gel filtration
Entamoeba histolytica
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
5.4.2.12
2-phospho-D-glycerate
Entamoeba histolytica
-
3-phospho-D-glycerate
-
-
r
5.4.2.12
2-phospho-D-glycerate
Entamoeba histolytica HM1 IMSS
-
3-phospho-D-glycerate
-
-
r
5.4.2.12
3-phospho-D-glycerate
Entamoeba histolytica
-
2-phospho-D-glycerate
-
-
r
5.4.2.12
3-phospho-D-glycerate
Entamoeba histolytica HM1 IMSS
-
2-phospho-D-glycerate
-
-
r
Purification (Commentary) (protein specific)
EC Number
Commentary
Organism
5.4.2.12
Ni-NTA column chromatography
Entamoeba histolytica
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
5.4.2.12
2-phospho-D-glycerate
-
748541
Entamoeba histolytica
3-phospho-D-glycerate
-
-
-
r
5.4.2.12
2-phospho-D-glycerate
-
748541
Entamoeba histolytica HM1 IMSS
3-phospho-D-glycerate
-
-
-
r
5.4.2.12
3-phospho-D-glycerate
-
748541
Entamoeba histolytica
2-phospho-D-glycerate
-
-
-
r
5.4.2.12
3-phospho-D-glycerate
-
748541
Entamoeba histolytica HM1 IMSS
2-phospho-D-glycerate
-
-
-
r
Subunits (protein specific)
EC Number
Subunits
Commentary
Organism
5.4.2.12
monomer
1 * 64000, SDS-PAGE
Entamoeba histolytica