Roles of HDACs and HDAC Inhibitors in Human Cancers

Dear Colleagues,

Pathologic alterations in epigenetic regulation of gene function have been found to be essentially involved in cancer initiation, progression and metastasis. On molecular and cellular levels, aberrantly active epigenetic factors cause altered gene expression patterns especially linked to epithelial to mesenchymal transition (EMT) and chemo-resistance.

Modifications of histones such as histone de-/acetylation represent a major epigenetic regulatory mechanism and play a significant role in human cancerogenesis. Histone deacetylation processes are regulated by a group of enzymes called histone deacetylases (HDACs), categorized in four classes. Overexpression of HDACs has been reported in several human cancer types, making these enzymes an interesting new potential therapeutic target. HDACs do also regulate the acetylation status of a variety of other non-histone substrates, including key tumour oncogenetic and suppressive genes as wells as associated proteins.

Specific inhibition of HDACs promotes tumour cells to undergo apoptosis, and cell-based in vitro as well as in vivo studies have shown a number of other outcomes to result from Histone deactelyase inhibitor (HDI) treatment, including cell-cycle arrest, cell differentiation, anti-angiogenesis and autophagy. Therefore, HDIs represent a promising class of drugs with therapeutic implications in tumour research.

To date, four HDIs have already been approved as anticancer agents: Belinostat, panobinostat, romidepsin and vorinostat. Nevertheless, there is strong interest in increasing the understanding of the pharmacology and underlying mechanisms of action as well as the specific targets of HDIs. This will be helpful for optimizing these drugs and for the development of more agents, which specifically target malfunctioning HDACs. Other than that the detection of biomarkers to predict HDI treatment responsiveness is also a critical issue regarding this topic.

This Special Issue calls for the contribution of original research papers and reviews focusing on HDACs and the role of HDAC inhibition in human cancer therapies to provide both, an up-to-date overview of the current knowledge as well as a platform to present novel scientific results addressing the promising increasingly cited research field of epigenetics in cancer therapy.

Dr. Daniel Neureiter
Guest Editor

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