Target intelligence / Profile preview

Eicosanoid biosynthesis enzyme

Molecular classification
Enzyme, Oxidoreductase (subfamily for specific enzymes), Monooxygenase (CYP), Lyase (LOX)
01

Overview

Eicosanoid biosynthesis enzymes are a heterogeneous group of enzymes comprising cyclooxygenases (COX-1, COX-2: prostaglandin-endoperoxide synthases), lipoxygenases (5-LOX, 12-LOX, 15-LOX), cytochrome P450 monooxygenases, and phospholipase A2 (PLA2)[1][3][5][7][9]. These enzymes mediate the conversion of polyunsaturated fatty acids into eicosanoids—prostaglandins, thromboxanes, leukotrienes, lipoxins, and specialized pro-resolving lipid mediators—which play central roles in both normal physiology (homeostasis, vascular tone, platelet function) and pathology (pain, fever, inflammation, cancer, cardiovascular disease, asthma, allergy, and infection)[4][5][7][9]. Many widely used anti-inflammatory and analgesic drugs, especially NSAIDs and COX-2 selective inhibitors, exert their therapeutic effects by inhibiting these enzymes, but safety concerns around gastrointestinal and cardiovascular side effects persist. The enzymes within this group represent proven and important therapeutic targets, although the designation "Eicosanoid biosynthesis enzymes" requires further specification to indicate exactly which enzyme is involved in any given context.

Other names
Eicosanoid pathway enzymesEicosanoid synthesis enzymesAA-metabolizing enzymes
02

Mechanism of action

Enzyme inhibition (blocking COX, LOX, or CYP enzymes reduces specific eicosanoid production) Acetylation (aspirin acetylates COX-1, inhibiting thromboxane A2 synthesis) Selective isoform inhibition (COX-2 inhibitors target inflammation while sparing homeostatic functions)[2][4][8][10]

03

Biological functions

Inflammation regulationImmune response modulationVascular tone regulationPlatelet aggregationHomeostasis (especially gastric, renal, and cardiovascular systems)
04

Disease associations

InflammationCancerCardiovascular disease (e.g., thrombosis, atherosclerosis, hypertension)Neurodegenerative diseaseAsthma and allergyInfectionPain
05

Safety considerations

Gastrointestinal toxicity (ulceration and bleeding with NSAIDs)Cardiovascular risk (blood clotting, increased thrombosis with COX-2 selective inhibitors)Impaired kidney function (long-term NSAID use)Hypersensitivity reactions (LOX inhibitors: risk of bronchospasm, especially in asthmatic patients)Immune system modulation risks
06

Interacting drugs

Aspirin (acetylates COX enzymes, principally COX-1 and COX-2)

7 more in the full profile.

07

Biomarkers

Prostaglandin E2 (PGE2) levelsThromboxane B2 (TXB2) levelsLeukotriene B4 (LTB4) levelsLipoxin A4 (LXA4) levels5-HETE, 12-HETE, 15-HETE, and EETs

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