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Target intelligence / Profile preview
20-Hydroxyeicosatetraenoic Acid (20-HETE)
- Target
- 20-HETE
- Molecular classification
- Eicosanoid, Hydroxy monocarboxylic acid, HETE (hydroxyeicosatetraenoic acids), Lipid Metabolite
01
Overview
20-Hydroxyeicosatetraenoic acid (20-HETE) is a potent vasoactive eicosanoid derived from arachidonic acid. It plays a crucial role in regulating vascular tone, blood flow, and sodium/fluid transport, particularly in the kidneys and brain. Its synthesis is catalyzed by cytochrome P450 enzymes (CYP4A and CYP4F). 20-HETE interacts with GPR75. Dysregulation of 20-HETE production or signaling is implicated in various diseases, including hypertension, stroke, metabolic syndrome, and cancer. It represents a potential therapeutic target for managing these conditions.
- Other names
- 20-hydroxy-5Z,8Z,11Z,14Z-eicosatetraenoic acid20-hydroxy arachidonic acid20-hydroxyarachidonic acid
02
Mechanism of action
Acts as a potent vasoconstrictor in renal, cerebral, mesenteric arteries by depolarizing vascular smooth muscle cells through inhibition of Ca²⁺–activated K⁺ channels and direct effects on L-type Ca²⁺ channels. High-affinity receptor identified as GPR75. The interaction between 20-HETE and GPR75 mediates many downstream bioactions
03
Biological functions
Vascular tone regulationBlood flow regulationSodium and fluid transport regulationVascular remodelingVasoconstrictionGPR75 signaling
04
Disease associations
HypertensionRenovascular diseaseGlomerular injuryIschemia/reperfusion injuryPolycystic kidney diseaseStrokeNeurovascular dysfunctionMetabolic syndromeDiabetesBreast cancerHereditary spastic paraplegiaCardiovascular disease
05
Safety considerations
Overproduction linked to hypertension-induced glomerular injury and renovascular disease statesMay contribute to certain cancersDeficiency associated with stroke risk/neurovascular dysfunctionsImplicated in metabolic syndrome/diabetes development/progressionLoss-of-function mutations can cause hereditary spastic paraplegia
06
Interacting drugs
Angiotensin II
3 more in the full profile.
07
Biomarkers
Urinary 20-HETE levelsBlood pressure changesVascular function
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