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Literature summary for 3.3.2.6 extracted from

  • Tholander, F.; Muroya, A.; Roques, B.P.; Fournie-Zaluski, M.C.; Thunnissen, M.M.; Haeggstroem, J.Z.
    Structure-based dissection of the active site chemistry of leukotriene A4 hydrolase: implications for M1 aminopeptidases and inhibitor design (2008), Chem. Biol., 15, 920-929.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli JM101 cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
mutant enzyme E296Q in complex with inhibitors RB3040 and RB3041, and substrate, liquid-liquid diffusion method, using 28% (w/v) polyethylene glycol, 50 mM Na acetate, 100 mM imidazole (pH 6.8), and 5 mM YbCl3 Homo sapiens

Protein Variants

Protein Variants Comment Organism
D375A mutant with reduced activity Homo sapiens
E296Q mutant with severely reduced activity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(S)-2-((S)-2-(2-(((R)-1-amino-2-phenylethyl)(hydroxy)phosphoryl)acetamido)-3-phenylpropanamido)-3-phenylpropanoic acid RB3041, tight slow-binding LTA4H inhibitor Homo sapiens
(S)-2-((S)-2-(2-(((R)-1-aminoethyl)(hydroxy)phosphoryl)acetamido)-3-(biphenyl-4-yl)propanamido)propanoic acid RB3040, tight slow-binding LTA4H inhibitor Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.3
-
Arg-Ser-Arg wild type enzyme, 500 mM KCl in 250 mM Tris buffer (pH 7.5) Homo sapiens
1.5
-
L-Arg-p-nitroanilide wild type enzyme, 500 mM KCl in 250 mM Tris buffer (pH 7.5) Homo sapiens
1.9
-
L-Ala-p-nitroanilide mutant enzyme E296Q, 500 mM KCl in 250 mM Tris buffer (pH 7.5) Homo sapiens
1.9
-
L-Ala-p-nitroanilide wild type enzyme, 500 mM KCl in 250 mM Tris buffer (pH 7.5) Homo sapiens
2.2
-
L-Arg-p-nitroanilide mutant enzyme E296Q, 500 mM KCl in 250 mM Tris buffer (pH 7.5) Homo sapiens
3
-
L-Ala-p-nitroanilide mutant enzyme D375A, 500 mM KCl in 250 mM Tris buffer (pH 7.5) Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ the enzyme contains zinc Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P09960
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Arg-Ala-Arg + H2O
-
Homo sapiens ?
-
?
Arg-Ser-Arg + H2O
-
Homo sapiens ?
-
?
L-Ala-p-nitroanilide + H2O
-
Homo sapiens L-Ala + p-nitroaniline
-
?
L-Arg-p-nitroanilide + H2O
-
Homo sapiens L-Arg + p-nitroaniline
-
?
leukotriene A4 + H2O
-
Homo sapiens leukotriene B4
-
?

Synonyms

Synonyms Comment Organism
leukotriene A4 hydrolase
-
Homo sapiens
LTA4H
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.001
-
L-Ala-p-nitroanilide mutant enzyme E296Q, 500 mM KCl in 250 mM Tris buffer (pH 7.5) Homo sapiens
0.002
-
L-Arg-p-nitroanilide mutant enzyme E296Q, 500 mM KCl in 250 mM Tris buffer (pH 7.5) Homo sapiens
0.5
-
L-Ala-p-nitroanilide mutant enzyme D375A, 500 mM KCl in 250 mM Tris buffer (pH 7.5) Homo sapiens
0.56
-
Arg-Ser-Arg wild type enzyme, 500 mM KCl in 250 mM Tris buffer (pH 7.5) Homo sapiens
1.7
-
L-Ala-p-nitroanilide wild type enzyme, 500 mM KCl in 250 mM Tris buffer (pH 7.5) Homo sapiens
1.9
-
L-Arg-p-nitroanilide wild type enzyme, 500 mM KCl in 250 mM Tris buffer (pH 7.5) Homo sapiens