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The Central Role of Cytochrome P450 in Xenobiotic Metabolism—A Brief Review on a Fascinating Enzyme Family

Center for Toxicogenomics and Human Health (ToxOmics), Genetics, Oncology and Huma Toxicology, NOVA Medical School/Faculty of Medical Sciences, Universidade NOVA de Lisboa, 1169-056 Lisboa, Portugal
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Academic Editor: François Gagné
J. Xenobiot. 2021, 11(3), 94-114; https://doi.org/10.3390/jox11030007
Received: 10 May 2021 / Revised: 14 June 2021 / Accepted: 16 June 2021 / Published: 22 June 2021
Human Cytochrome P450 (CYP) enzymes constitute a superfamily of membrane-bound hemoproteins that are responsible for the metabolism of a wide variety of clinically, physiologically, and toxicologically important compounds. These heme-thiolate monooxygenases play a pivotal role in the detoxification of xenobiotics, participating in the metabolism of many structurally diverge compounds. This short-review is intended to provide a summary on the major roles of CYPs in Phase I xenobiotic metabolism. The manuscript is focused on eight main topics that include the most relevant aspects of past and current CYP research. Initially, (I) a general overview of the main aspects of absorption, distribution, metabolism, and excretion (ADME) of xenobiotics are presented. This is followed by (II) a background overview on major achievements in the past of the CYP research field. (III) Classification and nomenclature of CYPs is briefly reviewed, followed by (IV) a summary description on CYP’s location and function in mammals. Subsequently, (V) the physiological relevance of CYP as the cornerstone of Phase I xenobiotic metabolism is highlighted, followed by (VI) reviewing both genetic determinants and (VI) nongenetic factors in CYP function and activity. The last topic of the review (VIII) is focused on the current challenges of the CYP research field. View Full-Text
Keywords: Cytochrome P450 (CYP); drug-metabolizing enzymes (DMEs); xenobiotic; metabolism; toxicology; carcinogens; adverse drug reactions (ADRs) Cytochrome P450 (CYP); drug-metabolizing enzymes (DMEs); xenobiotic; metabolism; toxicology; carcinogens; adverse drug reactions (ADRs)
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MDPI and ACS Style

Esteves, F.; Rueff, J.; Kranendonk, M. The Central Role of Cytochrome P450 in Xenobiotic Metabolism—A Brief Review on a Fascinating Enzyme Family. J. Xenobiot. 2021, 11, 94-114. https://doi.org/10.3390/jox11030007

AMA Style

Esteves F, Rueff J, Kranendonk M. The Central Role of Cytochrome P450 in Xenobiotic Metabolism—A Brief Review on a Fascinating Enzyme Family. Journal of Xenobiotics. 2021; 11(3):94-114. https://doi.org/10.3390/jox11030007

Chicago/Turabian Style

Esteves, Francisco, José Rueff, and Michel Kranendonk. 2021. "The Central Role of Cytochrome P450 in Xenobiotic Metabolism—A Brief Review on a Fascinating Enzyme Family" Journal of Xenobiotics 11, no. 3: 94-114. https://doi.org/10.3390/jox11030007

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