Journal
CURRENT MEDICINAL CHEMISTRY
Volume 10, Issue 19, Pages 1955-1972Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/0929867033456855
Keywords
cytochromes P450; drug metabolism; substrate selectivity
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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 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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