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High-Throughput Automated Multiplex Immunofluorescence Assays for Translational Research
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Multiplexing a high-throughput liability assay to leverage efficiencies.

John Herbst1, Monique Anthony, Jeremy Stewart

  • 1Lead Discovery, Profiling & Compound Management, Research and Development, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.

Assay and Drug Development Technologies
|June 18, 2009
PubMed
Summary
This summary is machine-generated.

This study optimized a high-throughput assay to detect drug-metabolizing enzyme inducers early in drug discovery. The new multiplexed assay efficiently measures pregnane X receptor (PXR) transactivation and cell viability simultaneously.

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Area of Science:

  • Pharmacology
  • Drug Discovery
  • Biochemistry

Background:

  • Cytochrome P-450 3A4 (CYP3A4) is a key drug-metabolizing enzyme.
  • Early identification of CYP3A4 inducers is crucial in drug discovery.
  • Pregnane X receptor (PXR) is a primary regulator of CYP3A4 expression.

Purpose of the Study:

  • To optimize a cell-based assay for identifying potential CYP3A4 inducers.
  • To develop a multiplexed assay combining PXR transactivation and cytotoxicity detection.
  • To improve efficiency and data quality in early drug discovery profiling.

Main Methods:

  • Implemented a high-throughput luciferase reporter assay for human PXR in HepG2 cells.
  • Applied Lean Thinking principles for lab-bench assay optimization and automation.
  • Developed a 384-well multiplexed homogeneous assay detecting PXR transactivation and cytotoxicity.
  • Optimized assay parameters including cell density, plate type, and reagent concentrations for multiplexing fluorescent and luminescent read-outs.

Main Results:

  • A validated multiplexed assay simultaneously detects PXR transactivation and HepG2 cell cytotoxicity.
  • Results from the multiplexed assay correlate well with singleplexed assays for PXR transactivation and viability.
  • The optimized assay demonstrates improved data quality, sample conservation, cost savings, and resource efficiencies.

Conclusions:

  • The multiplexed PXR transactivation and viability assay is suitable for routine compound profiling.
  • This optimized assay enables early-stage identification of potential drug-metabolizing enzyme inducers.
  • The developed assay enhances efficiency and data reliability in the drug discovery process.