Cytochrome P450 family 2 subfamily J member 2 (CYP2J2)

Cytochrome P450 family 2 subfamily J member 2 (CYP2J2) is an enzyme of the cytochrome P450 superfamily that localizes mainly to the endoplasmic reticulum and is highly expressed in the human heart, with lower levels in liver, intestine, kidney, lung, pancreas, brain, and other tissues[1][5][6]. CYP2J2 catalyzes the oxidation of endogenous polyunsaturated fatty acids—most notably converting arachidonic acid into epoxyeicosatrienoic acids (EETs), and also metabolizes linoleic acid, docosahexaenoic acid, and eicosapentaenoic acid to their respective epoxide derivatives[1][2][5]. These EETs regulate vascular tone, promote cardioprotection, modulate inflammation, and have roles in metabolic and proliferative signaling[1][2][5]. CYP2J2 is also involved in the Phase I metabolism of various drugs (e.g., astemizole, ebastine, amiodarone, rivaroxaban) and xenobiotics, with substrate selectivity and regioselectivity distinct from other P450 enzymes[3][6]. Overexpression is observed in several cancers, where CYP2J2 activity enhances cell proliferation and protects against apoptosis[1][5]; upregulation or downregulation contributes to cardiovascular and metabolic diseases[2][4][5]. Genetic polymorphisms may affect enzyme activity and disease risk. CYP2J2 is a potential therapeutic target for cardiovascular, metabolic, and oncological drug development, but is also a source of clinically significant drug–drug interactions and genetic variability in drug response[2][3][5][6].

Other names

Cytochrome P450 2J2Albendazole monooxygenase (hydroxylating)Albendazole monooxygenase (sulfoxide-forming)Arachidonic acid epoxygenaseCYPIIJ2Hydroperoxy icosatetraenoate isomeraseCPJ2Cytochrome P450, subfamily IIJ (arachidonic acid epoxygenase) polypeptide 2Flavoprotein-linked monooxygenaseMicrosomal monooxygenase

Drug metabolism via hydroxylation, epoxidation, or sulfoxidation (Phase I biotransformation) Generation of signaling metabolites (e.g., EETs) from arachidonic acid Competitive inhibition by certain drugs (e.g., danazol is a nanomolar inhibitor)