PXR and AhR nuclear receptor activation screening

The Pregnane X Receptor (PXR) and Aryl hydrocarbon Receptor (AhR) are nuclear transcriptional regulators that modulate the activity of cytochrome P450 genes. P450s code for metabolizing enzymes with central roles in organism protection against potential harmful agents. PXR and AhR are activated by binding diverse, but specific group of compounds (drugs, steroids, dioxin...). We offer a cell-based screening service to identify NCEs with the ability to modulate cytochromes CYP3A4 or CYP1A2 activity.

Identify PXR nuclear receptor activation agents

• Quantitation of receptor activation in stable human DPX2 cell line harboring a specific PXR-regulated reporter gene with a CYP3A4 promoter
• Synchronized quantitation of endogenous CYP3A4 enzyme substrate metabolism (optional)
• Determination of cell viability following incubation with NCE

Identify AhR nuclear receptor activation agents

• Quantitation of receptor activation in stable human 1A2-DRE cell line harboring a specific AhR-regulated reporter gene with a CYP1A2 promoter
• Synchronized quantitation of endogenous CYP1A2 enzyme substrate metabolism (optional)
• Determination of cell viability following incubation with NCE

Project management

• Process expertise
  Steps are customisable and allow for complete project outsourcing in an ISO9001-2008 certified quality management environment
• Complete transparency
  Project updates are provided weekly by a designated Project Manager and a specific Sales Manager is available for business interactions
• No strings attached
  Process methods are made available to customers for fast and efficient industrial exploitation with preservation of IP rights

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