Abstract
The mammalian sirtuins (SIRTs), comprising seven members (SIRT1–7) with different cellular localization, play crucial roles in the maintenance of proper cellular functions, appropriate responses against stress, and regulation of homeostatic and metabolic processes. However, mounting evidence is revealing the contrasting roles of SIRTs in cancer, either as a tumor suppressor or as an oncogene. Moreover, the emergence of SIRTs as potential cancer therapeutic candidates has led to the development of various SIRT inhibitors and activators in an attempt to control SIRT levels. Despite the wide range of available SIRT modulators, many lack selectivity and the requisite pharmacological properties and do not display a significant potency, ultimately limiting their potential for development as therapeutic agents. This chapter will discuss the roles of mammalian SIRTs in tumorigenesis and the development of SIRT modulators as anticancer agents.
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