Target intelligence / Profile preview

Lipoxygenase and cyclooxygenase enzymes (LOX and COX (also PTGS for cyclooxygenase in genetics))

Target
LOX and COX (also PTGS for cyclooxygenase in genetics)
Molecular classification
Enzyme, Oxidative enzyme, Iron-containing enzyme (LOX), Hemoprotein (COX), Member of arachidonic acid metabolizing enzyme family
01

Overview

Lipoxygenase and cyclooxygenase enzymes are responsible for the first committed steps in the arachidonic acid cascade, converting polyunsaturated fatty acids into a complex array of bioactive lipid mediators called eicosanoids[1][2][7]. Lipoxygenases are non-heme iron-containing enzymes that catalyze dioxygenation of fatty acids to produce hydroperoxides, which are then transformed into leukotrienes, lipoxins, and other signaling molecules[1][4]. Cyclooxygenases (COX, also called prostaglandin-endoperoxide synthases/PTGS) are hemoproteins that produce prostanoids including prostaglandins, thromboxanes, and prostacyclins[2][3]. These enzymes are central to the regulation of inflammation, immune signaling, and multiple other physiological processes[4][5]. Both families are important therapeutic targets, with numerous clinically approved drugs modulating their activities to control diseases such as pain, inflammation, cancer, and cardiovascular conditions[2][5][7]. The phrase "Lipoxygenase-cyclooxygenase pathway enzymes" is not the canonical form; it generically references two distinct enzyme families that should be considered separately for precise scientific and therapeutic purposes.

Other names
LOXlipoxygenasesCOXcyclooxygenasesprostaglandin-endoperoxide synthase (PTGS)prostaglandin G/H synthasearachidonate 5-lipoxygenase12-lipoxygenase15-lipoxygenaseCOX-1 (PTGS1)COX-2 (PTGS2)cyclooxygenase-1cyclooxygenase-2
02

Mechanism of action

Inhibition of enzyme catalytic activity, preventing formation of inflammatory lipid mediators. Selective isozyme inhibition (COX-1 vs COX-2; 5-LOX vs others). Substrate-selective inhibition and biosynthetic crossover.

03

Biological functions

Eicosanoid biosynthesisLipid mediator productionRegulation of inflammationCell signalingImmune responseCell proliferation and differentiationCellular homeostasis
04

Disease associations

InflammationCancer (including pancreatic cancer)Cardiovascular diseaseNeurodegenerative diseasesAsthma and allergic conditionsOther immune-mediated diseases
05

Safety considerations

Gastrointestinal ulceration and bleeding (COX-1 inhibition)Cardiovascular risks (selective COX-2 inhibition)Hepatotoxicity and other off-target effects (lipoxygenase inhibitors)
06

Interacting drugs

Non-steroidal anti-inflammatory drugs (NSAIDs: ibuprofen, aspirin, indomethacin) (COX inhibitors)

4 more in the full profile.

07

Biomarkers

Prostaglandins (PGE2, PGD2, etc.)Leukotrienes (LTB4, LTC4, etc.)5-HETE, 12-HETE, 15-HETE (hydroxy products of lipoxygenase activity)

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