Promega Corporation




Promega @cademy


Homepage

Previous Webinars

Other Tools

Contact

Ask a Scientist

Ask Customer Service

Promega @cademy: Recording/Presentation Request Form

Information

As ADME assays are performed earlier in drug discovery, the numbers of test compounds increases as does the need for predictive assays that are rapid, sensitive, cost effective and simple to perform. A novel bioluminescent assay format will be described that overcomes conventional limitations concerning one or more of these criteria. The simple add and read approach employs luciferase pro-substrates as activity probes for drug metabolizing enzymes that convert them to a product that generates light with luciferase in direct proportion to the enzyme activity of interest. An extensive collection of these drug-like probes with selectivity for a wide range of enzymes has now been synthesized. They are used in several cytochrome P450 (CYP), monoamine oxidase, N-acetyl transferase, UDP glucuronosyl transferase (UGT) and glutathione transferase (GST) assays. Cell free biochemical assays are used to screen for enzyme specific inhibitors and cell based CYP assays are used to measure induction in hepatocytes. The luminogenic assays produce IC50s for enzyme inhibition and EC50s for CYP induction that correlate well with conventional assays in terms of rank order and absolute potency. The cell-based CYP3A4 enzyme assay is compatible with orthogonal measurements such as CYP1A2, CYP3A4 transcriptional induction and cell viability. These multiplex approaches stream line data collection while improving data quality,
strengthening interpretation and removing ambiguity. This bioluminescent ADME assay suite provides an efficient approach to the discovery phase of drug development.


View recording

Thank you for your request for the Promega @cademy Recording/Presentation. To download the recording, please fill out and submit the following form. You will receive an email with the URL where you can download the recording and the presentation.


Entries with * are required.
First Name *
Last Name*
Institution *
Department
Street Address *
Bldg/Room
PO Box Address is for:
City *
State/Region
Country * Postal Code
Telephone Fax
E-Mail *
   
If you recently moved, help us stay current - please tell us where you were before!
Previous Institution Moved here
I give Promega or an authorized Promega distributor permission to contact me at the addresses that I provide.
 
     

Prefer a different language?

Your country is set to {0}
Your language is set to {1}

Select the language that will best suit your needs:

Continue

I need additional help »

  • Warning
  • It appears that you have Javascript disabled. Our website requires Javascript to function correctly. Please enable Javascript to experience our website.