School of Chemistry and Biomedical Sciences Research Complex, University of St. Andrews, North Haugh, St. Andrews, Fife, UK.
Bioorg Med Chem. 2012 Mar 1;20(5):1779-93. doi: 10.1016/j.bmc.2012.01.001. Epub 2012 Jan 12.
The tenovins are small molecule inhibitors of the NAD(+)-dependent family of protein deacetylases known as the sirtuins. There remains considerable interest in inhibitors of this enzyme family due to possible applications in both cancer and neurodegenerative disease therapy. Through the synthesis of novel tenovin analogues, further insights into the structural requirements for activity against the sirtuins in vitro are provided. In addition, the activity of one of the analogues in cells led to an improved understanding of the function of SirT1 in cells.
Tenovin 是一种小分子 NAD(+)依赖性蛋白去乙酰化酶家族（即 Sirtuins）抑制剂。由于这种酶家族可能在癌症和神经退行性疾病治疗方面具有应用前景，因此对其抑制剂仍存在浓厚的研究兴趣。通过合成新型的 tenovin 类似物，对体外针对 Sirtuins 的活性的结构要求有了更深入的了解。此外，其中一个类似物在细胞中的活性提高了我们对 SirT1 在细胞中的功能的认识。
