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Related Experiment Videos

Complex gel permeation assays for screening combinatorial libraries.

M E Schurdak1, M J Voorbach, L Gao

  • 1Department of Biological Screening, Abbott Laboratories, Abbott Park, IL 60064-3500, USA. mark.schurdak@abbott.com

Journal of Biomolecular Screening
|November 2, 2001
PubMed
Summary
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Gel permeation assays efficiently screen compound libraries for drug discovery. This study details three novel assays, including a neuraminidase inhibitor screen, discovering new acyclic neuraminidase inhibitors.

Area of Science:

  • Biochemistry
  • Drug Discovery
  • Assay Development

Background:

  • Gel permeation assays are standard for screening solid-supported combinatorial libraries.
  • Developing complex assays is crucial for high-throughput screening (HTS) operations.

Purpose of the Study:

  • To report three distinct gel permeation assays for screening compound libraries.
  • To demonstrate the adaptability of gel permeation assays for complex biological targets.
  • To identify novel inhibitors for influenza neuraminidase.

Main Methods:

  • Utilized gel permeation chromatography for library screening.
  • Developed a simple enzymatic assay for neuraminidase inhibitors.
  • Created complex ligand-receptor assays for interleukin-8 (IL-8)/IL-8 receptor and urokinase/urokinase receptor interactions.

Related Experiment Videos

  • Incorporated cell-based and ELISA-type formats into gel permeation assays.

    • Main Results:

    • Successfully screened combinatorial libraries using gel permeation assays.
    • Identified a novel series of acyclic inhibitors targeting influenza neuraminidase.
    • Demonstrated the feasibility of complex assays, including cell-based and ELISA formats, within a gel permeation framework.
    • Validated the utility of these assays in high-throughput screening.

    Conclusions:

    • Gel permeation assays can be adapted for complex biological targets beyond simple enzymatic assays.
    • This methodology enables routine screening of diverse compound collections against various targets.
    • The developed assays are valuable tools for drug discovery and HTS operations.