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Literature summary extracted from

  • Torres, M.J.; Fierro, A.; Pessoa-Mahana, C.D.; Romero-Parra, J.; Cabrera, G.; Faundez, M.
    Effect of alpha lipoic acid on leukotriene A4 hydrolase (2017), Eur. J. Pharmacol., 799, 41-47 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.3.2.6 (R)-5-(1,2-dithiolan-3-yl) pentanoic acid i.e. alpha-lipoic acid, inhibits both activities of the enzyme at concentrations lower than 0.010 mM. The carboxylate group of alpha lipoic acid situates at 3 A from important residues R563 and K565 in the catalytic pocket of the protein, suggesting that alpha lipoic acid participates in electrostatic interactions with these residues Homo sapiens
3.3.2.6 methyl 5-(1,2-dithiolan-3-yl) pentanoate i.e. alpha-lipoic acid methyl ester or LAME Homo sapiens
3.3.2.6 additional information 5-lipoxygenase inhibitor zileuton, or the 5-lipoxygenase activating protein inhibitor MK-886, are unable to inhibit the activity of the enzyme. Inhibitor docking and molecular dynamics simulations, interaction analysis Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.3.2.6 Zn2+ leukotriene A4 hydrolase is a zinc metalloenzyme Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.3.2.6 leukotriene A4 + H2O Homo sapiens
-
 leukotriene B4
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.3.2.6 Homo sapiens P09960
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.3.2.6 HL-60 cell
-
 Homo sapiens
-
3.3.2.6 macrophage
-
 Homo sapiens
-
3.3.2.6 neutrophil
-
 Homo sapiens
-
3.3.2.6 T-lymphocyte
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.3.2.6 leukotriene A4 + H2O
-
 Homo sapiens leukotriene B4
-
 ?
3.3.2.6 additional information substrates docking and molecular dynamics simulations, interaction analysis. The binding cavity of LTA4H is formed by H299, H295, E318, and Zn2+. Residues R563 and K565 in the C-terminal domain of LTA4H are key residues involved in carboxylate recognition from endogenous substrates of the enzyme Homo sapiens ?
-
 ?
3.3.2.6 proline-glycine-proline + H2O PGP Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.3.2.6 leukotriene A4 hydrolase
-
 Homo sapiens
3.3.2.6 LTA4H
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.3.2.6 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.3.2.6 7.4 8 assay at Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.3.2.6 0.00023
-
 pH 7.4, 37°C Homo sapiens (R)-5-(1,2-dithiolan-3-yl) pentanoic acid

General Information

EC Number General Information Comment Organism
3.3.2.6 malfunction imbalances in leukotriene B4 synthesis are related to several pathologic conditions Homo sapiens
3.3.2.6 metabolism leukotriene A4 hydrolase participates in the metabolism of lipid mediators and peptides Homo sapiens
3.3.2.6 additional information the enzyme has two catalytic pockets, a hydrophobic domain that recognizes the lipophilic hydrocarbon chain of LTA4 and a hydrophilic domain that recognizes the N-terminal region of PGP. Both domains converge in a common catalytic zone where the carboxylate group of each substrate interacts with alkaline amino acids in the protein. Thus, different catalytic pockets for separate activities share a carboxylate group recognition zone Homo sapiens
3.3.2.6 physiological function leukotriene A4 hydrolase is a soluble enzyme with epoxide hydrolase and aminopeptidase activities catalysing the conversion of leukotriene A4 to leukotriene B4 and the hydrolysis of the peptide proline-glycine-proline. Bifunctional LTA4H shows two catalytic activities, aminopeptidase activity hydrolysing the tripeptide proline-glycine-proline (PGP), and epoxide hydrolase activity on leukotriene A4 (LTA4) generating leukotriene B4 (LTB4), a potent inducer of macrophage, T-lymphocyte and neutrophil chemotaxis Homo sapiens