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Anticancer Agents Med Chem. 2016;16(8):1003-1016. doi: 10.2174/1871520616666160310141622.

Sirtuin Inhibitors: An Overview from Medicinal Chemistry Perspective.

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Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Minden, 11800, Penang, Malaysia.


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.


Histone deacetylases; cancer; epigenetic; inhibitor; sirtuin

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