BRENDA - Enzyme Database

Inhibition of human muscle-specific enolase by methylglyoxal and irreversible formation of advanced glycation end products

Pietkiewicz, J.; Gamian, A.; Staniszewska, M.; Danielewicz, R.; J. Enzyme Inhib. Med. Chem. 24, 356-364 (2009)

Data extracted from this reference:

General Stability
EC Number
General Stability
Organism
4.2.1.11
the enzyme maintains only 5% of the initial catalytic activity upon glycation for the first 90 min
Homo sapiens
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
4.2.1.11
methylglyoxal
incubation of0.015 mM enzyme with 2 mM, 3.1 mM and 4.34 mM methylglyoxal in 100 mM phosphate buffer pH 7.4 for 3 h causes the loss a 32%, 55% and 82% of initial specific activity, respectively. Inhibition of enolase by methylglyoxal and formation of enolase-derived glycation products arises more effectively in slight alkaline conditions and in the presence of inorganic phosphate
Homo sapiens
KM Value [mM]
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
4.2.1.11
0.2
-
2-phospho-D-glycerate
native enzyme, in the absence of methyglyoxal, in 50 mM imidazole-HCl buffer, pH 6.8, with 0.4 M KCl and 3 mM MgSO4
Homo sapiens
4.2.1.11
0.58
-
phosphoenolpyruvate
native enzyme, in the absence of methyglyoxal, in 50 mM imidazole-HCl buffer, pH 6.8, with 0.4 M KCl and 3 mM MgSO4
Homo sapiens
4.2.1.11
0.66
-
2-phospho-D-glycerate
glycated enzyme, in the presence of 40% (v/v) methyglyoxal, in 50 mM imidazole-HCl buffer, pH 6.8, with 0.4 M KCl and 3 mM MgSO4
Homo sapiens
4.2.1.11
0.83
-
phosphoenolpyruvate
glycated enzyme, in the presence of 40% (v/v) methyglyoxal, in 50 mM imidazole-HCl buffer, pH 6.8, with 0.4 M KCl and 3 mM MgSO4
Homo sapiens
Metals/Ions
EC Number
Metals/Ions
Commentary
Organism
Structure
4.2.1.11
Mg2+
required for activity, the optimum concentration is 3 mM
Homo sapiens
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
4.2.1.11
Homo sapiens
-
-
-
Source Tissue
EC Number
Source Tissue
Commentary
Organism
Textmining
4.2.1.11
skeletal muscle
-
Homo sapiens
-
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
4.2.1.11
2-phospho-D-glycerate
-
704848
Homo sapiens
phosphoenolpyruvate + H2O
-
-
-
r
pH Optimum
EC Number
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
4.2.1.11
6.8
-
-
Homo sapiens
General Stability (protein specific)
EC Number
General Stability
Organism
4.2.1.11
the enzyme maintains only 5% of the initial catalytic activity upon glycation for the first 90 min
Homo sapiens
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
4.2.1.11
methylglyoxal
incubation of0.015 mM enzyme with 2 mM, 3.1 mM and 4.34 mM methylglyoxal in 100 mM phosphate buffer pH 7.4 for 3 h causes the loss a 32%, 55% and 82% of initial specific activity, respectively. Inhibition of enolase by methylglyoxal and formation of enolase-derived glycation products arises more effectively in slight alkaline conditions and in the presence of inorganic phosphate
Homo sapiens
KM Value [mM] (protein specific)
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
4.2.1.11
0.2
-
2-phospho-D-glycerate
native enzyme, in the absence of methyglyoxal, in 50 mM imidazole-HCl buffer, pH 6.8, with 0.4 M KCl and 3 mM MgSO4
Homo sapiens
4.2.1.11
0.58
-
phosphoenolpyruvate
native enzyme, in the absence of methyglyoxal, in 50 mM imidazole-HCl buffer, pH 6.8, with 0.4 M KCl and 3 mM MgSO4
Homo sapiens
4.2.1.11
0.66
-
2-phospho-D-glycerate
glycated enzyme, in the presence of 40% (v/v) methyglyoxal, in 50 mM imidazole-HCl buffer, pH 6.8, with 0.4 M KCl and 3 mM MgSO4
Homo sapiens
4.2.1.11
0.83
-
phosphoenolpyruvate
glycated enzyme, in the presence of 40% (v/v) methyglyoxal, in 50 mM imidazole-HCl buffer, pH 6.8, with 0.4 M KCl and 3 mM MgSO4
Homo sapiens
Metals/Ions (protein specific)
EC Number
Metals/Ions
Commentary
Organism
Structure
4.2.1.11
Mg2+
required for activity, the optimum concentration is 3 mM
Homo sapiens
Source Tissue (protein specific)
EC Number
Source Tissue
Commentary
Organism
Textmining
4.2.1.11
skeletal muscle
-
Homo sapiens
-
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
4.2.1.11
2-phospho-D-glycerate
-
704848
Homo sapiens
phosphoenolpyruvate + H2O
-
-
-
r
pH Optimum (protein specific)
EC Number
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
4.2.1.11
6.8
-
-
Homo sapiens