Discovering Inhibitors of Human Sirtuin Type 2: Novel Structural Scaffolds

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• 作者：Anu J. Tervo ; Tiina Suuronen ; Sergiy Kyrylenko ; Erkki Kuusisto ; Pä ; ivi H. Kiviranta ; Antero Salminen ; Jukka Leppä ; nen ; Antti Poso
• 刊名：Journal of Medicinal Chemistry
• 出版年：2006
• 出版时间：November 30, 2006
• 年：2006
• 卷：49
• 期：24
• 页码：7239 - 7241
• 全文大小：134K
• 年卷期：v.49,no.24(November 30, 2006)
• ISSN：1520-4804

文摘

A successful virtual screening experiment of novel SIRT2 inhibitors is described. Four out of 11experimentally tested compounds showed in vitro inhibitory activity toward SIRT2 in a micromolar level,resulting in an experimental hit ratio of 36%. Two of these compounds inhibited SIRT2 with IC₅₀ (M)values of 51 and 91; moreover, one of the new inhibitors was comprised of an entirely new SIRT2-inhibitingstructural scaffold.