Target intelligence / Profile preview

Cytochrome P450 family 2 subfamily J member 3 (CYP2J3) (CYP2J3)

Target
CYP2J3
Molecular classification
Enzyme, Oxidoreductase, Cytochrome P450, Monooxygenase
01

Overview

Cytochrome P450 2J3 (CYP2J3) is a membrane-bound hemoprotein and a member of the cytochrome P450 superfamily, serving as the primary rat ortholog of the human CYP2J2 enzyme. It is predominantly expressed in the heart, vascular endothelium, and gastrointestinal tract, where it functions as a major epoxygenase. The enzyme's primary biological role is the epoxidation of arachidonic acid into four regioisomeric epoxyeicosatrienoic acids (EETs), which are potent signaling molecules that regulate vascular tone, inflammation, and cellular homeostasis. CYP2J3 also participates in the 25-hydroxylation of Vitamin D3 and the metabolism of various xenobiotics, including therapeutic drugs like astemizole and ebastine. In preclinical models, modulation of CYP2J3 expression has shown therapeutic potential for treating hypertension, insulin resistance, and myocardial ischemia-reperfusion injury. However, its role in drug metabolism also presents challenges related to drug-drug interactions and potential cardiotoxicity upon inhibition. As a key enzyme in the epoxygenase pathway, CYP2J3 is a vital subject for studying the physiological effects of eicosanoids and for developing novel cardiovascular therapies.

Other names
Arachidonic acid epoxygenaseCPJ3Cytochrome P450 2J3CYPIIJ3
02

Mechanism of action

Enzyme inhibition, Metabolic substrate

03

Biological functions

Lipid metabolismXenobiotic metabolismSignal transductionCardioprotectionVasodilationVitamin D metabolism
04

Disease associations

Cardiovascular diseaseHypertensionDiabetes mellitusInflammationCancer
05

Safety considerations

CardiotoxicityDrug-drug interactionsPromotion of tumor growth
06

Interacting drugs

Astemizole

7 more in the full profile.

07

Biomarkers

Epoxyeicosatrienoic acids (EETs)Dihydroxyeicosatrienoic acids (DHETs)Creatine kinase-MB (CK-MB)

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