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Leukotriene synthesis enzyme

Molecular classification
Enzyme, Oxidoreductase (for 5-lipoxygenase), Hydrolase (for LTA4 hydrolase), Transferase (for LTC4 synthase, MGST2)
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Overview

Leukotriene synthesis enzymes are a group of cytosolic and membrane-bound enzymes that catalyze the conversion of arachidonic acid to leukotrienes, which are potent immune-modulating lipid mediators[1][8]. Key enzymes include cytosolic phospholipase A2α (which releases arachidonic acid from phospholipids), 5-lipoxygenase (5-LOX), 5-lipoxygenase-activating protein (FLAP), LTA4 hydrolase, and LTC4 synthase[1][6]. These enzymes are primarily expressed in myeloid and other immunocompetent cells, assemble at the nuclear or perinuclear membranes upon cell activation, and jointly produce the leukotrienes LTB4 (a chemoattractant for neutrophils), LTC4, LTD4, and LTE4 (cysteinyl leukotrienes involved in bronchoconstriction and inflammatory responses)[1][6]. Pharmacological inhibition of one or more of these enzymes is established in asthma and allergy therapy and is under investigation for other chronic inflammatory and neoplastic diseases[2][8]. However, "Leukotriene synthesis enzymes" is not a single standardized target, but a descriptive group encompassing several defined molecular entities (such as 5-lipoxygenase, LTA4 hydrolase, and LTC4 synthase); therefore, the term is too broad and not strictly correct as a canonical single-target name[1][8].

Other names
Leukotriene biosynthetic enzymeLeukotriene-synthesizing enzymeEnzymes in leukotriene biosynthesis
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Mechanism of action

Enzyme inhibition (block leukotriene biosynthesis to reduce inflammatory signaling)

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Biological functions

Inflammatory mediator synthesisImmune responseSignal transduction
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Disease associations

InflammationAsthmaAllergic diseasesCardiovascular diseaseNeurodegenerative diseaseCancer
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Safety considerations

Off-target effects with general aminopeptidase inhibitorsPotential interference with host defense mechanisms
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Interacting drugs

Zileuton (5-lipoxygenase inhibitor)

5 more in the full profile.

07

Biomarkers

Leukotriene levels (e.g., LTB4, LTC4, LTD4 in biological fluids)Expression/activity of biosynthetic enzymes (e.g., 5-lipoxygenase, LTA4 hydrolase)

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