Cytochrome P450 Enzymes and Drug Metabolism in Humans

Human cytochrome P450 (CYP) enzymes, as membrane-bound hemoproteins, play important roles in the detoxification of drugs, cellular metabolism, and homeostasis. In humans, almost 80% of oxidative metabolism and approximately 50% of the overall elimination of common clinical drugs can be attributed to...

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Bibliographic Details
Published in:International journal of molecular sciences Vol. 22; no. 23; p. 12808
Main Authors: Zhao, Mingzhe, Ma, Jingsong, Li, Mo, Zhang, Yingtian, Jiang, Bixuan, Zhao, Xianglong, Huai, Cong, Shen, Lu, Zhang, Na, He, Lin, Qin, Shengying
Format: Journal Article
Language:English
Published: Switzerland MDPI AG 26.11.2021
MDPI
Subjects:
Animals
Cancer therapies
Clinical outcomes
Cytochrome
Cytochrome P-450 Enzyme System - genetics
Cytochrome P-450 Enzyme System - metabolism
Drugs
Enzymes
Epigenetics
Humans
Inactivation, Metabolic
Ligands
Metabolic Clearance Rate
Metabolism
Metabolites
Pharmaceutical Preparations - metabolism
Pharmaceuticals
Polymorphism, Genetic
Review
Xenobiotics - metabolism
protein structure
cytochrome P450
genetic polymorphisms
drug metabolism
ISSN:1422-0067, 1661-6596, 1422-0067
Online Access:Get full text
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Summary:Human cytochrome P450 (CYP) enzymes, as membrane-bound hemoproteins, play important roles in the detoxification of drugs, cellular metabolism, and homeostasis. In humans, almost 80% of oxidative metabolism and approximately 50% of the overall elimination of common clinical drugs can be attributed to one or more of the various CYPs, from the CYP families 1–3. In addition to the basic metabolic effects for elimination, CYPs are also capable of affecting drug responses by influencing drug action, safety, bioavailability, and drug resistance through metabolism, in both metabolic organs and local sites of action. Structures of CYPs have recently provided new insights into both understanding the mechanisms of drug metabolism and exploiting CYPs as drug targets. Genetic polymorphisms and epigenetic changes in CYP genes and environmental factors may be responsible for interethnic and interindividual variations in the therapeutic efficacy of drugs. In this review, we summarize and highlight the structural knowledge about CYPs and the major CYPs in drug metabolism. Additionally, genetic and epigenetic factors, as well as several intrinsic and extrinsic factors that contribute to interindividual variation in drug response are also reviewed, to reveal the multifarious and important roles of CYP-mediated metabolism and elimination in drug therapy.
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These authors equally contributed to this work.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms222312808