Cytochrome P450 family 4 subfamily F member 3 (CYP4F3)
Target
CYP4F3
Molecular classification
Enzyme, Cytochrome P450 monooxygenase
01
Overview
Cytochrome P450 family 4 subfamily F member 3 (CYP4F3) is a human enzyme of the cytochrome P450 superfamily, primarily involved in the omega-oxidation of various fatty acids and bioactive lipids, including leukotriene B4 and arachidonic acid[1][2][5]. CYP4F3 exists in multiple tissue-specific isoforms (CYP4F3A and CYP4F3B), with distinct substrate preferences: CYP4F3A is mainly in leukocytes and inactivates leukotriene B4, a key inflammatory mediator, whereas CYP4F3B predominates in the liver and converts arachidonic acid into 20-hydroxyeicosatetraenoic acid (20-HETE), a lipid regulator of vascular tone and blood pressure[1][2][5]. Genetic variants in CYP4F3 are linked to susceptibility for inflammatory diseases and possibly modulate host responses to infection[1]. CYP4F3 activity influences inflammation resolution, fatty acid degradation, and vascular physiology and has regulatory roles in several disease states through lipid mediator metabolism[1][2][5].
Drugs targeting CYP4F3 would act through inhibition or modulation of its omega-oxidation activity, affecting the metabolism of leukotriene B4 and potentially 20-HETE synthesis[1][2][5].
03
Biological functions
Drug metabolismOmega-oxidation of fatty acidsInactivation and degradation of inflammatory mediators (e.g., leukotriene B4)Synthesis of lipid regulators (e.g., 20-HETE)
04
Disease associations
InflammationCardiovascular disease (implicated via regulation of blood pressure and vascular tone)Cancer (involvement suggested via lipid mediator regulation)Inflammatory bowel diseaseTrichuriasis (associated per genetic linkage)
05
Safety considerations
Potential off-target effects impacting metabolism of other endogenous substrates (lipids, drugs)Modulation of inflammatory mediator breakdown could pose risks for immune responses and cardiovascular effectsGenetic polymorphisms may alter enzyme activity and affect individual responses to drugs or susceptibility to inflammatory diseases[1][2]
06
Interacting drugs
No specific drugs directly targeting CYP4F3 are currently well-characterized. However, drugs that affect the cytochrome P450 enzyme family or leukotriene pathways may be relevant in indirect interactions[1][2].
07
Biomarkers
Single nucleotide polymorphisms (SNPs) in CYP4F3, such as rs1290617, rs1290620, rs1290622, rs1290625, and rs3794987, have been studied for association with Crohn's disease, celiac disease, and viral susceptibility[1].Expression levels of CYP4F3A or CYP4F3B in leukocytes or liver tissue may serve as inflammatory or metabolic biomarkers[1][2][5].
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