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Identification of Four Potential Epigenetic Modulators from the NCI Structural Diversity Library Using a Cell-Based Assay

  1. Author:
    Best, A. M.
    Chang, J. J.
    Dull, A. B.
    Beutler, J. A.
    Martinez, E. D.

  2. Author Address

    [Best, Anne M.; Chang, Jianjun; Martinez, Elisabeth D.] Univ Texas SW Med Ctr Dallas, Dept Pharmacol, Dallas, TX 75390 USA. [Best, Anne M.; Chang, Jianjun; Martinez, Elisabeth D.] Univ Texas SW Med Ctr Dallas, Hamon Ctr Therapeut Oncol Res, Dallas, TX 75390 USA. [Dull, Angie B.] NCI, Mol Targets Lab, Ctr SAIC Frederick, Frederick, MD 21702 USA. [Beutler, John A.] NCI, Mol Targets Lab, Ctr Canc Res, Dallas, TX 75390 USA.;Martinez, ED, Univ Texas SW Med Ctr Dallas, Dept Pharmacol, 6000 Harry Hines Blvd, Dallas, TX 75390 USA.;elisabeth.martinez@utsouthwestern.edu
    1. Year: 2011
  2. Journal: Journal of Biomedicine and Biotechnology
    1. Pages: 11
  4. Type of Article: Article
  5. Article Number: 868095
  6. ISSN: 1110-7243
  1. Abstract:

    Epigenetic pathways help control the expression of genes. In cancer and other diseases, aberrant silencing or overexpression of genes, such as those that control cell growth, can greatly contribute to pathogenesis. Access to these genes by the transcriptional machinery is largely mediated by chemical modifications of DNA or histones, which are controlled by epigenetic enzymes, making these enzymes attractive targets for drug discovery. Here we describe the characterization of a locus derepression assay, a fluorescence-based mammalian cellular system which was used to screen the NCI structural diversity library for novel epigenetic modulators using an automated imaging platform. Four structurally unique compounds were uncovered that, when further investigated, showed distinct activities. These compounds block the viability of lung cancer and melanoma cells, prevent cell cycle progression, and/or inhibit histone deacetylase activity, altering levels of cellular histone acetylation.

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External Sources

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  2. DOI: 10.1155/2011/868095
  3. View record in Web of Science®
  4. WOS: 000286248100001

Library Notes

  1. Fiscal Year: FY2011-2012
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