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Related Experiment Videos

Target validation in drug discovery.

Robert A Blake1

  • 1Exelixis, Inc., South San Francisco, CA, USA.

Methods in Molecular Biology (Clifton, N.J.)
|September 22, 2006
PubMed
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High content screening (HCS) aids early-stage pharmaceutical target validation, particularly with genetic methods like RNA interference (RNAi). This approach enables efficient assay development and in-depth analysis for oncology targets.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Target validation is crucial for identifying viable pharmaceutical targets.
  • High content screening (HCS) offers valuable throughput and in-depth analysis for early-stage target validation.
  • Genetic methods, including RNA interference (RNAi), are increasingly used in target validation.

Purpose of the Study:

  • To illustrate the application of HCS in early-stage target validation.
  • To demonstrate efficient assay development for signaling pathways.
  • To showcase the simultaneous measurement of multiple cellular events.

Main Methods:

  • Utilized high content screening (HCS) for target validation in oncology.
  • Employed RNA interference (RNAi) for genetic manipulation.

Related Experiment Videos

  • Developed assays to measure specific molecular targets within signaling pathways, such as the Akt pathway.
  • Combined phenotypic assays measuring proliferation and apoptosis in single cells.

    • Main Results:

    • Demonstrated an efficient method for identifying HCS-compatible reagents using the Akt pathway.
    • Described an HCS assay capable of simultaneously measuring Akt substrate and RPS6 phosphorylation.
    • Illustrated the combined measurement of DNA synthesis and apoptosis in the same cell population.

    Conclusions:

    • HCS is a powerful tool for early-stage target validation, especially when combined with genetic methods like RNAi.
    • The developed assays enable simultaneous measurement of multiple pathway nodes and phenotypic markers.
    • This integrated approach facilitates robust assessment of molecular targets for therapeutic development.