Epigenetics Protocols

Volume 791 of the series Methods in Molecular Biology pp 297-311


Inhibition of Histone Deacetylases

  • Yi HuangAffiliated withUniversity of Pittsburgh Cancer Institute
  • , Patrick G. ShawAffiliated withUniversity of Pittsburgh Cancer Institute
  • , Nancy E. DavidsonAffiliated withUniversity of Pittsburgh Cancer Institute Email author 

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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.

Key words

Histone deacetylases Histone acetyltransferases HDAC inhibitors Epigenetic gene silencing Chromatin remodeling