UGT Induction
The potential for drug-drug interactions to affect the pharmacological profile of new chemical entities has necessitated a thorough detection into possible common causes, one of which is enzyme induction. At present, the majority of the investigations on induction have focused on the CYP enzymes, while investigations involving the UGT enzymes have been limited.
UGTs are a superfamily of membrane-bound enzymes that detoxify a large amount of endogenous and exogenous compounds. Until now, 15 functionally active human UGTs have been characterized and classified into two subfamilies (UGT1 and UGT2) based on amino acid sequence similarity.
Of all the isoforms, UGT1A1, UGT1A9, and UGT2B7 are available for induction assays. Creative Bioarray is providing these assays for your drug development needs.
UGT induction assay protocol
| Test Concentration | 0, 0.25, 0.5, 1, 2, 5, 10, 25μM (or other concentrations) |
| Enzymes | UGT1A1, UGT1A9, UGT2B7 |
| Time Points | 0, 5, 15, 30, 45, 60, 120 minutes |
| Number of Replicates | n=3 per time point |
| Analysis Method | Enzymatic activity: LC-MS/MS or fluorescent quantification mRNA levels: qPCR |
Creative Bioarray has an experienced team and state-of-the-art equipment to provide you with quality service. If you have any questions or special needs in reaction phenotyping service, please contact us.
Reference
- Soars MG, Wrighton SA. An assessment of udp-glucuronosyltransferase induction using primary human hepatocytes. Drug Metab Dispos. 2004 Jan;32(1):140-8.
