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Literature summary for 1.1.1.21 extracted from

  • Balendiran, G.K.; Rajkumar, B.
    Fibrates inhibit aldose reductase activity in the forward and reverse reactions (2005), Biochem. Pharmacol., 70, 1653-1663.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
overexpression of His-tagged enzyme in Escherichia coli strain BL21 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
bezafibrate noncompetitive, IC50: 0.003 mM, recombinant enzyme Homo sapiens
ciprofibrate competitive, IC50: 0.00086 mM, recombinant enzyme Homo sapiens
Clofibric acid noncompetitive, IC50: 0.0012 mM, recombinant enzyme Homo sapiens
fenofibrate competitive, IC50: 0.00056 mM, recombinant enzyme Homo sapiens
gemfibrozil noncompetitive, IC50: 0.0065 mM, recombinant enzyme Homo sapiens
sorbinil competitive, IC50: 0.0021 mM, recombinant enzyme Homo sapiens
zopolrestat competitive, IC50: 0.00006 mM, recombinant enzyme Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information kinetics Homo sapiens
0.092
-
DL-glyceraldehyde pH 6.2, 25°C, recombinant enzyme Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged enzyme from Escherichia coli strain BL21 by metal affinity chromatography, removal of the His-tag by thrombin, and anion exchange chromatography to homogeneity Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
placenta
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyl alcohol + oxidized 3-acetylpyridine adenine dinucleotide + H+
-
Homo sapiens benzaldehyde + reduced 3-acetylpyridine adenine dinucleotide
-
r
DL-glyceraldehyde + NADPH + H+
-
Homo sapiens glycerol + NADP+
-
r

Synonyms

Synonyms Comment Organism
aldose reductase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.76
-
DL-glyceraldehyde pH 6.2, 25°C, recombinant enzyme Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
additional information
-
pH preference depends on the substrate Homo sapiens
6.2
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Homo sapiens
NADPH
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics, pH dependence of inhibition, overview Homo sapiens
0.000043
-
zopolrestat pH 6.2, 25°C, recombinant enzyme Homo sapiens
0.00045
-
sorbinil pH 6.2, 25°C, recombinant enzyme Homo sapiens
0.00056
-
fenofibrat pH 6.2, 25°C, recombinant enzyme Homo sapiens
0.00088
-
ciprofibrate pH 6.2, 25°C, recombinant enzyme Homo sapiens
0.0011 0.0026 bezafibrate pH 6.2, 25°C, recombinant enzyme Homo sapiens
0.0012 0.0037 gemfibrozil pH 6.2, 25°C, recombinant enzyme Homo sapiens
0.00124
-
Clofibric acid pH 6.2, 25°C, recombinant enzyme Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00006
-
competitive, IC50: 0.00006 mM, recombinant enzyme Homo sapiens zopolrestat
0.00056
-
competitive, IC50: 0.00056 mM, recombinant enzyme Homo sapiens fenofibrate
0.00086
-
competitive, IC50: 0.00086 mM, recombinant enzyme Homo sapiens ciprofibrate
0.0012
-
noncompetitive, IC50: 0.0012 mM, recombinant enzyme Homo sapiens Clofibric acid
0.0021
-
competitive, IC50: 0.0021 mM, recombinant enzyme Homo sapiens sorbinil
0.003
-
noncompetitive, IC50: 0.003 mM, recombinant enzyme Homo sapiens bezafibrate
0.0065
-
noncompetitive, IC50: 0.0065 mM, recombinant enzyme Homo sapiens gemfibrozil