UGT Inhibition (and Other Non-CYP Enzymes)

The majority of drug-drug interactions (DDI) occur at the metabolic level. This physiological process usually changes the activity of metabolic enzymes such as UGT. The identification of UGT inhibition is highlighted as one of the main evaluations for the candidate compounds.

UGT inhibition assay, although performed less than CYP assay, still plays an important role in the DDI experiments. Because UGT inhibition may cause toxic side-effects.

Creative Bioarray provides UGT inhibition assays available for isoforms 1A1, 1A3, 1A4, 1A6, 1A9, 2B7, and 2B15. Our team uses recombinant enzymes and different inhibitor concentrations to assess IC₅₀ values towards specific UGT isoforms.

Fig.1 Inhibitory effects of 1-naphthol on estradiol 3-O(A), imipramine N(B), serotonin O(C), or propofol -O(D) glucuronide formations in human liver microsome (HLM) and recombinant UGTs.¹

Supplementary Assays

Others non-CYP enzymes:

• Flavin containing mono-oxygenase (FMO)
• Monoamine-oxidase (MAO)
• Carboxylesterase (CE)
• Aldehyde oxidase (AOX)
• Xanthine oxidase (XO)
• Sulfotransferase (SULT)

Quotation and ordering

Our scientific team is committed to providing high quality service of UGT and other non-CYP enzymes assays for your candidate compounds. With extensive experience and professional knowledge, we promise to satisfy your requirements. If you have any special needs or questions regarding our services, do not hesitate to contact us to find out more about our services.

Reference

1. Fujiwara, R. (2008). “Product Inhibition of UDP-Glucuronosyltransferase (UGT) Enzymes by UDP Obfuscates the Inhibitory Effects of UGT Substrates.” Drug Metab Dispos 36(2), 361-367.

Explore Other Options

• In Vitro Metabolism
• In Vitro Permeability and Transporters
• Drug-Drug Interaction
• High-throughput ADME Screening
• Physicochemical Characterization Assays

• Cytochrome P450 Induction and Inhibition Assays
• Drug Transporters
• Hepatocyte Stability Assay
• Metabolite Identification
• Microsomal Stability Assay

For research use only. Not for any other purpose.