Metyrapone, cytochrome P450 inhibitor. Blocks cortisol synthesis.

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.

Activity summary

Cytochrome P450 3A4 often abbreviated as CYP3A4 is an enzyme of the cytochrome P450 superfamily. This enzyme has a mass approximately 57 kDa and functions as an important player in the oxidation of small organic molecules during drug metabolism. CYP3A4 is expressed in the liver which is its primary site of expression as well as in the intestine. An alternate enzyme name C11B2 or CYP11B2 sometimes refers to a distinct enzyme involved in steroid biosynthesis. However CYP3A4 is important for metabolizing compounds by facilitating the oxidation of substrates such as lipids and natural compounds.

Biological function summary

CYP3A4 metabolizes a wide range of drugs that are administered therapeutically. It is not part of a multimeric complex but acts on its own to catalyze metabolic reactions. This enzyme facilitates the conversion of lipophilic drugs into more hydrophilic metabolites which become easier for the body to excrete. Moreover CYP3A4 plays a role in steroid hormone biosynthesis contributing to processes like cortisol synthesis where it influences the cortisol molecular structure. The enzyme also participates in the metabolism of endogenous steroids like testosterone and progesterone.

Pathways

CYP3A4 functions centrally in the drug metabolism pathway which is fundamental for the detoxification and elimination of xenobiotics. Another significant pathway involving CYP3A4 is the synthesis and metabolism of cholesterol and steroid hormones. It interacts with proteins such as CYP2C9 which also metabolizes drugs and steroids to ensure chemical homeostasis within the body. These pathways rely heavily on the activity of cytochrome P450 enzymes highlighting their importance in various physiological processes.

Associated diseases and disorders

CYP3A4 activities can influence the development and management of conditions like liver disease and drug-induced toxicity. Overexpression or inhibition of this enzyme can lead to significant alterations in drug efficacy and safety affecting conditions like chronic liver diseases. In metabolic disorders the enzyme's normal functioning can be hampered influencing cortisol production and leading to imbalanced cortisol chemical structure. Additionally CYP3A4's activity relates to other enzymes such as CYP2D6 which also plays roles in the metabolism of pharmaceuticals and is implicated in metabolic syndrome.