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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

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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 Km and Ki values, respectively, are tabulated. Furthermore, physicochemical properties in the form of lipophilicity (log P and log D7.4 values) and acidity / basicity (pKa 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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Keywords: cytochromes p450; drug metabolism; substrate selectivity

Document Type: Review Article

Affiliations: School of Biomedical and Life Sciences, University of Surrey, Guildford, Surrey, GU2 7XH, UK.

Publication date: 01 October 2003

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