Histone deacetylases (HDACs) are a group of enzymes closely related to sirtuins. They catalyze the removal of acetyl groups from lysine residues in histones and non-histone proteins, resulting in transcriptional repression. In general, they do not act autonomously but as components of large multiprotein complexes, such as pRb-E2F and mSin3A, that mediate important transcription regulatory pathways.
There are three classes of HDACs; classes 1, 2 and 4, which are closely related Zn2+-dependent enzymes. HDACs are ubiquitously expressed and they can exist in the nucleus or cytosol. Their subcellular localization is affected by protein-protein interactions (for example HDAC-14.3.3 complexes are retained in the cytosol) and by the class to which they belong (class 1 HDACs are predominantly nuclear whilst class 2 HDACs shuttle between the nucleus and cytosol). HDACs have a role in cell growth arrest, differentiation and death and this has led to substantial interest in HDAC inhibitors as possible antineoplastic agents.
Histone acetylation is upregulated during memory formation but downregulated in numerous neurodegenerative diseases, such as Alzheimer's disease and Huntington's disease. As a result, HDAC inhibitors are also of great interest in neuroscience research.View all products for Histone Deacetylases »
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Literature for Histone Deacetylases
Cancer Research Guide
A collection of over 350 products for cancer research, the guide contains modulators of:
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Cell Death and Drug Resistance
- Invasion and Metastasis
Epigenetics Research Bulletin
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. Their biological effects are also discussed. Compounds available from Tocris are listed.
Review excerpt: "While histone deacetylase (HDAC) inhibitors were discovered as early as 1978, other epigenetic proteins and their inhibitors have only recently become the focus of intensive research. Unrestricted access to well-characterized chemical probes has now opened up new areas of biological research and therapeutic possibilities."Request copy | Download PDF
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April 18 - 22, 2015