The β-NAD⁺-dependent N^ε-acyl-lysine deacylation reaction catalyzed by sirtuin family members has been increasingly demonstrated to be important in regulating multiple crucial cellular processes and has also been proposed to be a therapeutic target for multiple human diseases. Accordingly, its inhibitors have been actively pursued over the past few years. In addition, we have also seen the pharmacological assessment of sirtuin inhibitory compounds, although to a lesser extent. In this review, we first discuss how sirtuin inhibitors were discovered with the use of various approaches. We then follow with a discussion of pharmacological studies using sirtuin inhibitors. Our aim here is to set a stage for developing future superior sirtuin inhibitors and for an expanded effort in exploiting inhibitors to explore and/or validate the therapeutic potential stemming from the inhibition of the sirtuin-catalyzed deacylation reaction.

的β-NAD ⁺依赖性Ñ ^ε由sirtuin家族成员催化的α-酰基赖氨酸脱酰反应已日益证明在调节多种关键细胞过程中很重要，并且也被提议作为多种人类疾病的治疗靶标。因此，在过去的几年中一直积极地寻求其抑制剂。此外，尽管程度较轻，我们也看到了瑟土因抑制性化合物的药理学评估。在这篇综述中，我们首先讨论如何使用各种方法来发现瑟土因抑制剂。然后，我们讨论使用瑟土因抑制剂的药理研究。