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Related Experiment Videos

High-content fluorescence-based screening for epigenetic modulators.

Elisabeth D Martinez1, Angie B Dull, John A Beutler

  • 1Laboratory of Receptor Biology and Gene Expression, Hormone Action and Oncogenesis Section, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.

Methods in Enzymology
|November 18, 2006
PubMed
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This study details novel fluorescent assays for screening epigenetic modulators, targeting enzymes like histone deacetylases and DNA methyltransferases crucial for cancer therapy development.

Area of Science:

  • Molecular Biology
  • Epigenetics
  • Drug Discovery

Background:

  • Epigenetic processes regulate gene transcription and are implicated in diseases like cancer.
  • Aberrant epigenetic pathways highlight cellular enzymes as key therapeutic targets.
  • Histone deacetylases and DNA methyltransferases are critical epigenetic enzymes.

Purpose of the Study:

  • To develop and present mammalian cell-based fluorescent assays for screening epigenetic modulators.
  • To provide protocols for drug screening, hit characterization, and mechanism of action evaluation.
  • To discuss principles for selecting hit compounds for lead development in cancer research.

Main Methods:

  • Development of mammalian cell-based fluorescent assays.
  • Application of assays for screening epigenetic modulators.

Related Experiment Videos

  • Utilizing an innovative combination of approaches for assay development.

    • Main Results:

    • Established functional fluorescent assays for epigenetic modulators.
    • Provided detailed protocols for drug screening and hit characterization.
    • Presented methods for evaluating compound mechanism of action.

    Conclusions:

    • Mammalian cell-based fluorescent assays offer a viable method for screening epigenetic modulators.
    • These assays facilitate the identification and development of potential cancer therapeutics.
    • The developed protocols support the advancement of epigenetic drug discovery.