Detecting subtle activity modulation in drug discovery is often hampered by background noise in fluorescent systems. Avoid the limitations of fluorescence with Promega's range of homogeneous, luminescent ADME assays available for measurement of cytochrome P450s, P-glycoprotein (Pgp) or monoamine oxidase (MAO).
Promega's new ADME assays are ideal for testing the effects of drugs and new chemical entities on P450s, Pgp and MAO activity. These assays enable biologically relevant data to be collected early in drug discovery, reducing late stage failures, saving time and money.
The P450-Glo? CYP450 Screening Assays are designed to measure the activities of P450s from recombinant and native sources. Systems are available for CYP1A2, CYP2C9, CYP3A4, CYP2C19 and CYP2D6. Each assay
system provides a complete set of reagents for performing luminescent P450 assays. P-glycoprotein (Pgp), an integral plasma membrane protein that functions as an ATPdependent drug efflux pump, is important in
drug absorption and distribution, and plays a key role in multi-drug resistance. Compounds that interact with Pgp can be identified as
stimulators or inhibitors of its ATPase activity.
Compounds that are substrates for transport by Pgp typically stimulate its ATPase activity. The Pgp-Glo? Assay detects the effects of compounds on recombinant human Pgp activity in a cell membrane fraction.
MAO-Glo? is another new addition to Promega's expanding range of ADME assays. The system provides all the reagents necessary to measure MAO A and B, which play a key role in biotransformation of amine containing compounds. Unlike HPLC or fluorometric methods, less MAO enzyme is required with MAO-Glo? because of the enhanced sensitivity afforded by luminescence.
The P450-Glo? Assay Systems, Pgp-Glo? and MAO-Glo? are all amenable to automation and offer excellent Z'- factor values.
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