The role of sirtuins in age-related diseases is an area of rapidly expanding
investigation. Sirtuins are NAD+ -dependent class III histone deacetylases (HDACs) that share
extensive homologies with the yeast HDAC Sir2. Class I and class II HDACs inhibitors have
been identified as potential anticancer agents and are in clinical studies, but much less is known
about class III HDAC inhibitors. However, inhibitors of sirtuins are currently being targeted as
potential therapeutic agents for disease such as cancer, neurodegenerative disease and other
disorders as sirtuins are discovered to regulate numerous downstream enzymes. Given the link
between sirtuins and cancer, understanding the functionality of these enzymes may ultimately
have significant impact in cancer prevention or cancer treatment. This review gives an updated
overview regarding the regulation of sirtuin enzymes, their implications in cancer, various
sirtuin inhibitor scaffolds and their insights in drug design.
Keywords: Histone deacetylases, sirtuin, inhibitor, epigenetic, cancer.
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