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Literature summary for 3.3.2.6 extracted from

  • Andberg, M.; Wetterholm, A.; Medina, J.F.; Haeggstrom, J.Z.
    Leukotriene A4 hydrolase: a critical role of glutamic acid-296 for the binding of bestatin (2000), Biochem. J., 345, 621-625.
No PubMed abstract available
Search for more literature for 3.3.2.6

Application

Application Comment Organism
medicine the enzyme catalyses the hydrolysis of leukotriene A4 into the proinflammatory substance leukotriene B4 Mus musculus

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli as a fusion protein with ten additional amino acids at the amino terminus Mus musculus

Protein Variants

Protein Variants Comment Organism
E296D decrease of inhibitor potency of bestatin in comparison to wild-type enzyme, but the inhibitor potencies of alpha-oxo-beta-amino carboxylic ester, a thioamine and amino hydroxamic acid is identical for mutant and wild-type enzyme Mus musculus
E296N decrease of inhibitor potency of bestatin in comparison to wild-type enzyme, but the inhibitor potencies of alpha-oxo-beta-amino carboxylic ester, a thioamine and amino hydroxamic acid is identical for mutant and wild-type enzyme Mus musculus
E296Q decrease of inhibitor potency of bestatin in comparison to wild-type enzyme, but the inhibitor potencies of alpha-oxo-beta-amino carboxylic ester, a thioamine and amino hydroxamic acid is identical for mutant and wild-type enzyme Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
2-oxo-3-amino carboxylic esters comparison of inhibition of mutant and wild-type enzymes Mus musculus
bestatin comparison of inhibition of mutant and wild-type enzymes, mechanism Mus musculus
hydroxamic acid comparison of inhibition of mutant and wild-type enzymes Mus musculus
thioamine comparison of inhibition of mutant and wild-type enzymes Mus musculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.001 0.005 leukotriene A4 pH 7.9, 22°C, mutant E296D Mus musculus
0.005
-
 leukotriene A4 pH 7.9, 22°C, wild-type enzyme Mus musculus
0.005
-
 leukotriene A4 pH 7.9, 22°C, mutant E296N Mus musculus
0.011
-
 leukotriene A4 pH 7.9, 22°C, mutant E296Q Mus musculus

Metals/Ions

Metals/Ions Comment Organism Structure
Zinc zinc protein Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Mus musculus

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.31
-
 mutant E296N Mus musculus
0.49
-
 mutant E296D Mus musculus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
leukotriene A4 + H2O
-
 Mus musculus leukotriene B4
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.9
-
 leukotriene A4 pH 7.9, 22°C, wild-type enzyme Mus musculus
1.4
-
 leukotriene A4 pH 7.9, 22°C, mutant E296Q Mus musculus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0007
-
 bestatin pH 7.9, 22°C, wild-type enzyme Mus musculus
0.021
-
 bestatin pH 7.9, 22°C, mutant E296Q Mus musculus