Cited by 255Pharmacogenetics and Drug MetabolismDrug Transport and Resistance MechanismsDrug-Induced Hepatotoxicity and Protection

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Reactions and enzymes in the metabolism of drugs and other xenobiotics

Testa, Bernard, Pedretti, Alessandro, Vistoli, Giulio·2012·Drug Discovery Today

DOI 10.1016/j.drudis.2012.01.017

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Abstract

In this article, we offer an overview of the compared quantitative importance of biotransformation reactions in the metabolism of drugs and other xenobiotics, based on a meta-analysis of current research interests. Also, we assess the relative significance the enzyme (super)families or categories catalysing these reactions. We put the facts unveiled by the analysis into a drug discovery context and draw some implications. The results confirm the primary role of cytochrome P450-catalysed oxidations and UDP-glucuronosyl-catalysed glucuronidations, but they also document the marked significance of several other reactions. Thus, there is a need for several drug discovery scientists to better grasp the variety of drug metabolism reactions and enzymes and their consequences.

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Authors: Testa, B., Pedretti, A., & Vistoli, G.
Affiliations: Centre Hospitalier Universitaire Vaudois (CH)
University of Milan (IT)
Corresponding author: Testa, Bernard
ORCID: Testa, Bernard
Pedretti, Alessandro
Vistoli, Giulio
Venue: Drug Discovery Today
Publisher: Elsevier BV
Published: 2012-06
Volume: 17
Issue: 11-12
Pages: 549-560
ISSN: 1359-6446 (ISSN-L)
DOI: 10.1016/j.drudis.2012.01.017
OpenAlex: W2075550795
Cited by: 254
References: 64
Citations by year: 2026: 14 · 2025: 24 · 2024: 23 · 2023: 30 · 2022: 19 · 2021: 28 · 2020: 21 · 2019: 10 · 2018: 12 · 2017: 19 · 2016: 9 · 2015: 17 · 2014: 17 · 2013: 6 · 2012: 4
FWCI: 2.62
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: Drug Discovery Today (publishedVersion)
PubMed (publishedVersion)
IRIS (submittedVersion)
SERVAL (Université de Lausanne) (submittedVersion)
Topics: Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Drug-Induced Hepatotoxicity and Protection
Keywords: drug metabolism, xenobiotic metabolism, cytochrome P450, UDP-glucuronosyltransferase, glucuronidation, drug-metabolizing enzymes, enzyme superfamilies, drug discovery
MeSH terms: Animals, Biochemical Phenomena, Pharmaceutical Preparations, Enzymes, Humans, Substrate Specificity, Xenobiotics, Molecular Structure, Metabolic Detoxication, Phase I, Metabolic Detoxication, Phase II, Drug Discovery, Drug-Related Side Effects and Adverse Reactions

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Reactions and enzymes in the metabolism of drugs and other xenobiotics

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