Guest Editors
Dr. Meran Keshawa Ediriweera, Department of Biochemistry and Molecular Biology, Faculty of Medicine, University of Colombo, Sri Lanka. meran@bmb.cmb.ac.lk
Dr. Dilusha Fernando, Department of Biochemistry and Molecular Biology, Faculty of Medicine, University of Colombo, Sri Lanka. dilusha@bmb.cmb.ac.lk
Summary
The term epigenetics refers to the heritable changes occurred in gene functions which cannot be allotted to variations in the DNA sequence. DNA methylation and histone modification play a crucial role in epigenetic modifications. Among the main post-translational histone modifications, histone acetylation is a well-controlled event which is maintained by the actions of histone acetyltransferases (HATs) and histone deacetylases (HDACs). Acetylation of ε-NH2 groups present on lysine residues by HATs results relaxation of chromatin and transcriptional activation. HDACs prevent the function of HATs by deacetylating histone lysine residues and thereby inducing transcriptional repression. As histone acetylation is well-maintained by the opposing actions of HATs and HDACs, it is evident that any irregularity in the actions of HATs and HDACs can result in the development of a range of human diseases including cancer.
Chromatin-modifying agents, which have the ability to correct irregularities in epigenetic markers, have gained much attention as a new class of anti-cancer therapeutics. Of them, histone deacetylase inhibitors (HDACi) are considered as a promising class as they can re-establish the irregularities in the acetylation profiles of cancer cells, allowing cancer cells to undergo programmed cell death. Based on the chemical groups/moieties present in the structures, HDACi can be classified into four major classes namely; benzamides, hydroxamic acids, cyclic tetrapeptides and short chain fatty acids. So far, a wide range of natural or synthetic HDACi acting on different HDACs (pan-HDACi) or isoform specific HDACi have been identified, and these HDACi allow researchers to investigate the possible roles of different HDACs in human cancer.
The present special issue welcomes original research articles, reviews, communications and future perspectives related to natural histone deacetylase inhibitors, molecular mechanisms and their potential therapeutic utility as anti-cancer agents.
Potential topics include but are not limited to the following:
• Natural histone deacetylase inhibitors
• Pre-clinical and clinical findings with histone deacetylase inhibitors
• Natural histone deacetylase inhibitor library screening
• In-silico findings
• Toxicity assessment of histone deacetylase inhibitors
• Novel classes of histone deacetylase inhibitors
• Natural and synthetic derivatives
Keywords
Histone Deacetylase Inhibitors, Cancer, Histone Acetyltransferases, Histone Deacetylases, Natural Drugs and Chromatin-Modifying Agents
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