Target intelligence / Profile preview

Cyclooxygenase and lipoxygenase enzyme (COX and LOX)

Target
COX and LOX
Molecular classification
Enzyme, Oxidoreductase
01

Overview

Cyclooxygenases and lipoxygenases are critical enzymes in the metabolism of polyunsaturated fatty acids, particularly arachidonic acid, to generate eicosanoids such as prostaglandins, thromboxanes, leukotrienes, and lipoxins[3][4][10]. Cyclooxygenase isoforms (COX-1 and COX-2) mediate the synthesis of prostanoids, which regulate processes such as inflammation, vascular homeostasis, and platelet function[10]. Lipoxygenases, with multiple isoforms (5-LOX, 12-LOX, 15-LOX, etc.), catalyze the formation of leukotrienes and other lipid mediators that modulate immune responses, inflammation resolution, and apoptosis[7][10]. Both enzyme families are key therapeutic targets for anti-inflammatory, anticancer, and cardiovascular therapies, and dual inhibition approaches are under investigation to improve efficacy and reduce side effects[3][4][5][9][10]. However, given the widely varied roles and isoforms, each should be specified carefully in research and clinical contexts.

Other names
Cyclooxygenase (COX)Lipoxygenase (LOX)COX-1 (Prostaglandin-endoperoxide synthase 1)COX-2 (Prostaglandin-endoperoxide synthase 2)5-LOX (ALOX5)12-LOX (ALOX12)15-LOX (ALOX15, ALOX15B)
02

Mechanism of action

Inhibition of prostaglandin synthesis (COX inhibition) Inhibition of leukotriene synthesis (LOX inhibition) Dual COX/5-LOX inhibition reduces both prostaglandin and leukotriene production, helps reduce cardiovascular and gastrointestinal side effects

03

Biological functions

Inflammation responseImmune modulationEicosanoid biosynthesis (prostaglandins, thromboxanes, leukotrienes, lipoxins)Cell proliferationCell survivalApoptosis/programmed cell deathAngiogenesisRegulation of vascular tone and platelet aggregation
04

Disease associations

Inflammation (rheumatoid arthritis, psoriasis, asthma)Cancer (pancreatic cancer, prostate cancer, other tumor types)Cardiovascular diseaseOther chronic inflammatory disorders
05

Safety considerations

GI toxicity and ulceration (COX inhibition, especially non-selective NSAIDs)Cardiovascular risk (COX-2 selective inhibitors)Hepatotoxicity and renal effectsDual inhibitors: high toxicity, low efficacy limited clinical use
06

Interacting drugs

Nonsteroidal anti-inflammatory drugs (NSAIDs, e.g., ibuprofen, aspirin – inhibit COX)

3 more in the full profile.

07

Biomarkers

Overexpression or upregulation of COX-2 (marker in various cancers)5-LOX expression/activity (associated with cancer and inflammatory disease)Levels of prostaglandins and leukotrienes

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