Target intelligence / Profile preview

Cytochrome P450 4A enzyme (CYP4A)

Target
CYP4A
Molecular classification
Enzyme, Monooxygenase, Heme protein, Oxidoreductase
01

Overview

The **Cytochrome P450 4A enzyme** (CYP4A) is a member of the large cytochrome P450 superfamily involved in the oxidative metabolism of fatty acids, drugs, and xenobiotics. It contains a conserved heme-iron active site responsible for oxygen activation and substrate hydroxylation. CYP4A enzymes are expressed in liver and kidney, where they participate in the ω-hydroxylation of medium- and long-chain fatty acids as well as eicosanoids, influencing physiological processes such as blood pressure regulation, lipid homeostasis, and inflammation. The enzymes are pharmacologically relevant due to their inducibility, broad substrate specificity, and involvement in drug metabolism and detoxification. Alterations in CYP4A function or expression are implicated in disease risk and therapeutic outcomes[2][3][1].

Other names
CYP4ACytochrome P450 family 4 subfamily AFatty acid ω-hydroxylase
02

Mechanism of action

Many drugs modify substrate hydroxylation or overall fatty acid metabolism by either inhibiting or inducing CYP4A enzymes, affecting drug clearance or metabolite production[2]. Mechanistic actions include direct competitive inhibition, enzyme induction, or modulation of enzyme expression by nuclear receptors.

03

Biological functions

Fatty acid metabolism (including ω-hydroxylation of fatty acids)Oxidative metabolism of xenobiotics/drugsRegulation of lipid homeostasisBioactivation and detoxication of endogenous and exogenous substrates
04

Disease associations

Cancer (altered expression and function implicated in certain cancers)Cardiovascular disease (linked to blood pressure regulation via fatty acid metabolism)Inflammation (modulates inflammatory eicosanoids such as 20-HETE)Metabolic syndrome (influences lipid and glucose metabolism)
05

Safety considerations

Drug-drug interactions (predicted or observed due to CYP4A’s role in drug metabolism)Toxic metabolite formation (potential for production of reactive intermediates, especially if CYP4A is over-induced)Individual variability (expression and activity of CYP4A varies with genotype, disease state, and induction/inhibition by drugs)
06

Interacting drugs

Clofibrate (inducer)

3 more in the full profile.

07

Biomarkers

CYP4A expression/activity in tissues (potential biomarker for metabolic or cardiovascular conditions)20-HETE levels (a key metabolite produced by CYP4A enzymes, used to monitor enzyme activity and associated disease risk)

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