CYP1A2

1. 본문

CYP1A2 (Cytochrome P450 1A2) is a member of the cytochrome P450 mixed-function oxidase system, a superfamily of enzymes that play a crucial role in the metabolism of various substances in the body. Here's a breakdown of what CYP1A2 is and its functions:
What it is:

• Enzyme: CYP1A2 is an enzyme, a type of protein that speeds up chemical reactions.
• Cytochrome P450 Family: It belongs to the cytochrome P450 (CYP) family, specifically subfamily 1A, member 2.
• Location: It's primarily found in the liver, localized to the endoplasmic reticulum.
• Gene: The *CYP1A2* gene encodes the CYP1A2 enzyme.

• Xenobiotic Metabolism: CYP1A2 is involved in the oxidative metabolism of xenobiotics, which are foreign compounds not naturally produced by the body, such as drugs and environmental chemicals.
• Drug Metabolism: It metabolizes a variety of clinically important drugs. Some specific examples of drugs metabolized by CYP1A2 include:
• Caffeine
• Theophylline
• Clozapine
• Olanzapine
• Tizanidine
• Amitriptyline
• Clomipramine
• Duloxetine
• Tacrine
• Procarcinogen Activation: It can metabolize some polycyclic aromatic hydrocarbons (PAHs), found in cigarette smoke, into carcinogenic (cancer-causing) intermediates.
• Endogenous Substrate Metabolism: While its primary role is in xenobiotic metabolism, CYP1A2 also metabolizes some endogenous substrates (substances naturally found in the body, including steroids, and arachidonic acid.
• Caffeine Metabolism: CYP1A2 is the main enzyme responsible for caffeine metabolism.
• Polyunsaturated Fatty Acid Metabolism: CYP1A2 metabolizes polyunsaturated fatty acids into signaling molecules.

• Induction: CYP1A2 expression can be induced (increased) by certain substances, most notably PAHs found in cigarette smoke. Omeprazole can also induce CYP1A2.
• Inhibition: Various substances can inhibit (decrease) CYP1A2 activity. Some potent inhibitors include:
• Fluvoxamine
• Ciprofloxacin
• Enoxacin
• Cimetidine
• Furafylline
• Genetic Variation: Genetic variations (polymorphisms) in the *CYP1A2* gene can affect enzyme activity, leading to interindividual differences in drug metabolism.
• Other factors: Non-genetic factors such as smoking, inflammation and cholestasis may also influence the expression of CYP1A2.

• Docking studies have identified Phe226, Ala317, Gly316, Phe125, and Thr124 as the most important residues to influence the inhibitory potency of the enzyme.