Affiliation:
1. National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Huazhong Agricultural University, Wuhan, Hubei 430070, China
Abstract
Human cytochrome P450 enzyme 1A2 (CYP1A2) is one of the most important cytochrome P450
(CYP) enzymes in the liver, accounting for 13% to 15% of hepatic CYP enzymes. CYP1A2 metabolises many
clinical drugs, such as phenacetin, caffeine, clozapine, tacrine, propranolol, and mexiletine. CYP1A2 also
metabolises certain precarcinogens such as aflatoxins, mycotoxins, nitrosamines, and endogenous substances
such as steroids. The regulation of CYP1A2 is influenced by many factors. The transcription of CYP1A2 involves
not only the aromatic hydrocarbon receptor pathway but also many additional transcription factors, and
CYP1A2 expression may be affected by transcription coactivators and compression factors. Degradation of
CYP1A2 mRNA and protein, alternative splicing, RNA stability, regulatory microRNAs, and DNA methylation
are also known to affect the regulation of CYP1A2. Many factors can lead to changes in the activity of
CYP1A2. Smoking, polycyclic aromatic hydrocarbon ingestion, and certain drugs (e.g., omeprazole) increase
its activity, while many clinical drugs such as theophylline, fluvoxamine, quinolone antibiotics, verapamil,
cimetidine, and oral contraceptives can inhibit CYP1A2 activity. Here, we review the drugs metabolised by
CYP1A2, the metabolic mechanism of CYP1A2, and various factors that influence CYP1A2 metabolism. The
metabolic mechanism of CYP1A2 is of great significance in the development of personalised medicine and
CYP1A2 target-based drugs.
Funder
National Key Research and Development Program of China
Publisher
Bentham Science Publishers Ltd.
Subject
Clinical Biochemistry,Pharmacology
Cited by
35 articles.
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