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Inhibition of Histone Deacetylases

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Epigenetics Protocols

Part of the book series: Methods in Molecular Biology ((MIMB,volume 791))

Abstract

Lysine acetylation of histones is one of the major epigenetic regulators of chromatin conformation and gene expression. The dynamic nature of histone acetylation is determined by the counterbalancing activity of histone acetyltransferase and histone deacetylase (HDAC) enzymes. Acetylation of histones is generally associated with open and transcriptionally active chromatin, whereas the activity of HDACs leads to histone deacetylation, condensation of chromatin, and inhibition of transcription. Aberrant silencing of tumor suppressors and other genes has been found in different types of cancer. Abnormal activity of HDACs has been implicated in tumorigenesis and therefore considerable effort has been put into the development of HDAC inhibitors as a means of modifying histone acetylation status and reexpressing aberrantly silenced tumor suppressor genes. This has led to the generation of a number of structurally diverse compounds that can effectively inhibit HDAC activity, thus altering chromatin structure in cancer cells. This unit discusses the methods and recent technological developments with respect to the studies of HDAC inhibition in cancer.

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Acknowledgments

This work was funded by NIH SPORE grant CA88843 (to N.E.D.) and the Breast Cancer Research Foundation (to N.E.D.).

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Authors and Affiliations

  1. University of Pittsburgh Cancer Institute, Pittsburgh, PA, USA

    Yi Huang, Patrick G. Shaw & Nancy E. Davidson

Authors
  1. Yi Huang
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  2. Patrick G. Shaw
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  3. Nancy E. Davidson
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Corresponding author

Correspondence to Nancy E. Davidson .

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Editors and Affiliations

  1. Dept. Biology, University of Alabama, Birmingham, University Blvd. 1300, Birmingham, 35294-1170, Alabama, USA

    Trygve O. Tollefsbol

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Huang, Y., Shaw, P.G., Davidson, N.E. (2011). Inhibition of Histone Deacetylases. In: Tollefsbol, T. (eds) Epigenetics Protocols. Methods in Molecular Biology, vol 791. Humana Press. https://doi.org/10.1007/978-1-61779-316-5_22

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  • DOI: https://doi.org/10.1007/978-1-61779-316-5_22

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  • Publisher Name: Humana Press

  • Print ISBN: 978-1-61779-315-8

  • Online ISBN: 978-1-61779-316-5

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