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These are the first examples of potential function polymorphisms resulting from missense mutations in the CgammaP3A4 gene. The CgammaP3A4*2 allele was found to encode a P450 with substrate-dependent altered kinetics compared with the wild-type P450.

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ABSTRACT:We have tested a panel of 29 cDNA-expressed rat and human enzymes with 9 fluorometric substrates to determine the P450 isoform selectivity in the catalysis of the substrates to fluorescent products. The substrates examined were dibenzyl fluorescein, 7-benzyloxyquinoline (BQ), 3-cyano-7-ethoxycoumarin, 3-cyano-7-methoxycoumarin, 7-methoxy-4-trifluoromethylcoumarin, 3- Cytochrome P450 (P450 1 ) enzymes are the principal enzymes that catalyze the metabolism of drugs and other xenobiotics. Analysis of drug metabolism by the cytochrome P450 system has become an important part of the drug discovery/development process, and numerous assay methodologies have been developed. Cytochrome P450 activity assays which have fluorometric endpoints are advantageous in that they offer high sensitivity and are often direct and homogeneous assays. These properties enable testing larger numbers of experimental conditions with cost effective, higher-throughput methodologies. Indeed, fluorometric P450 substrates have been used for many applications in toxicology and drug discovery and development (Ullrich and

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