Human Cytochromes P450 Associated with the Phase 1 Metabolism of Drugs and other Xenobiotics: A Compilation of Substrates and Inhibitors of the CYP1, CYP2 and CYP3 Families
Abstract
This review represents a compilation of typical substrates and inhibitors for human cytochrome P450 (CYP) enzymes that are involved in drug metabolism, specifically those from the CYP1, CYP2 and CYP3 families. Relatively recent literature on substrates and inhibitors has been collected and the relevant K(m) and K(i) values, respectively, are tabulated. Furthermore, physicochemical properties in the form of lipophilicity (log P and log D(7.4) values) and acidity/basicity (pK(a) values) are also tabulated for a significant number of substrates, together with some information on inhibitors, although only key inhibitors have been selected as the main focus is on substrates. The collated information indicates that there are certain commonalities between substrates for the same enzyme, especially with respect to their positions of metabolism and likely interactions with the relevant enzyme active site regions. The compilation therefore assists in establishing substrate structure-activity relationships (SSARs) within human drug-metabolizing P450s.
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[123I]5-IA is metabolized in the liver by enzymes in the cytochrome P450 family, such as CYP2A6, CYP2B6, and CYP2D6.
“Consistently, we expect that [123I]5-IA is metabolized in the liver by enzymes in the cytochrome P450 family, such as CYP2A6, which acts on nicotine, and CYP2B6 and CYP2D6, which catalyze the dealkylation of aromatic ethers56, 57.”
From β2-Nicotinic Acetylcholine Receptor Availability During Acute and Prolonged Abstinence From Tobacco Smoking (2009) · cites this paper as [57]
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- Authors
- Lewis, D.
- Affiliations
- University of Surrey (GB)
- Corresponding author
- Lewis, David
- Venue
- Current Medicinal Chemistry
- Publisher
- Bentham Science Publishers Ltd.
- Published
- 2003-10-01
- Volume
- 10
- Issue
- 19
- Pages
- 1955-1972
- ISSN
- 0929-8673 (ISSN-L)
- OpenAlex
- W2003222087
- Cited by
- 129
- References
- 0
- Citations by year
- 2026: 4 · 2025: 1 · 2024: 3 · 2023: 5 · 2022: 2 · 2021: 5 · 2020: 3 · 2019: 2 · 2018: 7 · 2017: 3 · 2016: 7 · 2015: 8 · 2014: 5 · 2013: 6 · 2012: 2
- FWCI
- 5.07
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Current Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- Funders
- GlaxoSmithKline
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Physical Sciences › Chemistry › Inorganic Chemistry › Metal-Catalyzed Oxygenation Mechanisms
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Keywords
- cytochrome P450, drug metabolism, xenobiotics, enzyme substrates, enzyme inhibitors, Michaelis constant, inhibition constant, lipophilicity, pKa, structure-activity relationship, enzyme active site
- MeSH terms
- Cytochrome P-450 Enzyme System, Pharmaceutical Preparations, Enzyme Inhibitors, Humans, Hydrogen Bonding, Protein Binding, Structure-Activity Relationship, Substrate Specificity, Xenobiotics, Molecular Structure, Cytochrome P-450 Enzyme Inhibitors
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