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Identification of Four Potential Epigenetic Modulators from the NCI Structural Diversity Library Using a Cell-Based Assay
Joint Authors
Chang, Jianjun
Martinez, Elisabeth D.
Dull, Angie B.
Beutler, John A.
Best, Anne M.
Source
Journal of Biomedicine and Biotechnology
Issue
Vol. 2011, Issue 2011 (31 Dec. 2011), pp.1-11, 11 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2010-12-22
Country of Publication
Egypt
No. of Pages
11
Main Subjects
Abstract EN
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.
American Psychological Association (APA)
Best, Anne M.& Chang, Jianjun& Dull, Angie B.& Beutler, John A.& Martinez, Elisabeth D.. 2010. Identification of Four Potential Epigenetic Modulators from the NCI Structural Diversity Library Using a Cell-Based Assay. Journal of Biomedicine and Biotechnology،Vol. 2011, no. 2011, pp.1-11.
https://search.emarefa.net/detail/BIM-504724
Modern Language Association (MLA)
Best, Anne M.…[et al.]. Identification of Four Potential Epigenetic Modulators from the NCI Structural Diversity Library Using a Cell-Based Assay. Journal of Biomedicine and Biotechnology No. 2011 (2011), pp.1-11.
https://search.emarefa.net/detail/BIM-504724
American Medical Association (AMA)
Best, Anne M.& Chang, Jianjun& Dull, Angie B.& Beutler, John A.& Martinez, Elisabeth D.. Identification of Four Potential Epigenetic Modulators from the NCI Structural Diversity Library Using a Cell-Based Assay. Journal of Biomedicine and Biotechnology. 2010. Vol. 2011, no. 2011, pp.1-11.
https://search.emarefa.net/detail/BIM-504724
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-504724