Non-CYP Mediated Metabolism
Carboxylesterase (CE) Inhibition Assay
Understand if your compound is an inhibitor of carboxylesterases.
Carboxylesterase (CE) inhibition is a non-CYP inhibition assay within our portfolio of in vitro ADME screening services. Cyprotex delivers consistent, high quality data with the flexibility to adapt protocols based on specific customer requirements.
Introduction
Determining potential inhibition of carboxylesterase enzymes:
- Human carboxylesterases (CE) are Phase I drug metabolizing enzymes of the serine hydrolase superfamily. They hydrolyse a variety of ester containing drugs and prodrugs.
- Carboxylesterase inhibitors may play a role in improved efficacy of compounds inactivated by this class of enzymes and/or reduce the toxicity of agents that are activated by these enzymes.
- Cyprotex’s carboxylesterase inhibition assay identifies if your compound is an inhibitor of the carboxylesterase (CE) isoform, hCE1, using hCE1-b and hCE1-c recombinant enzymes.
Protocol
Carboxylesterase Inhibition Assay Protocol
Data
Data from the Carboxylesterase (CE) Inhibition Assay
Figure 1
Inhibition of trandolapril (hCE1 substrate) metabolism in recombinant hCE1-b by benzil.
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Cyprotex enables and enhances the prediction of human exposure, clinical efficacy and toxicological outcome of a drug or chemical. By combining quality data from robust in vitro methods with contemporary in silico technology, we add value, context and relevance to the ADME-Tox data supplied to our partners in the pharmaceutical or chemical industries.
