Inhibition of histone deacetylases

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

Research output: Chapter in Book/Report/Conference proceedingChapter

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.

Original languageEnglish (US)
Title of host publicationEpigenetics Protocols
EditorsTrygve O. Tollefsbol
Pages297-311
Number of pages15
DOIs
StatePublished - Oct 24 2011

Publication series

NameMethods in Molecular Biology
Volume791
ISSN (Print)1064-3745

Keywords

  • Chromatin remodeling
  • Epigenetic gene silencing
  • HDAC inhibitors
  • Histone acetyltransferases
  • Histone deacetylases

ASJC Scopus subject areas

  • Molecular Biology
  • Genetics

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  • Cite this

    Huang, Y., Shaw, P. G., & Davidson, N. E. (2011). Inhibition of histone deacetylases. In T. O. Tollefsbol (Ed.), Epigenetics Protocols (pp. 297-311). (Methods in Molecular Biology; Vol. 791). https://doi.org/10.1007/978-1-61779-316-5_22