Drug metabolizing enzymes (DME) are a diverse group of enzymes located primarily in the liver. They metabolize vast array of xenobiotic compounds including drugs, environmental pollutants, and endogenous compounds such as steroids and prostaglandins.

Structure-activity relationships of drug metabolizing enzymes and their substrates comprise an important area of research that impacts pharmacology, toxicology and basic enzymology. There are increasing efforts to incorporate metabolism studies early in the drug discovery process because poor pharmacokinetics account for a substantial proportion of clinical failures. To accelerate these efforts, Life Technologies provides recombinant drug metabolizing enzymes and assay methods that enable scientists to screen large numbers of diverse compounds for their drug metabolism profiles.

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Cytochrome P450 BACULOSOMES® Plus Reagents are microsomes prepared from insect cells infected with recombinant baculovirus containing cDNA for a human P450 isozyme, human NADPH-P450 reductase, and in some cases human cytochrome b5. P450 BACULOSOMES® Plus Reagents offer a distinct advantage over human liver microsomes (HLMs), for targeted studies of P450 isoforms, because only one P450 is expressed. This prevents interfering metabolism by other P450s or other classes of DMEs.

Compound rankings based on metabolism and inhibition profiles observed with P450 BACULOSOMES® Plus Reagents are very similar to those seen with HLMs for most compounds tested. Activity and metabolic rates of the P450 BACULOSOMES® Plus Reagents with most substrates, however, is significantly higher than those observed from preparations of HLMs.

CYP3A4 Vivid Assays

Figure 1. CYP3A4 Vivid® Assays with BACULOSOMES® Plus Reagents correlate well with LC-UV assays. IC50 values for 12 known CYP3A4 inhibitors were obtained using four distinct Vivid® Substrates, and compared to values generated using a traditional testosterone 6 beta-hydroxylation LC-UV assay with CYP3A4 BACULOSOMES® Plus Reagent. The Vivid® Assays were highly predictive of LC-UV assay results.