Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases
- 作者：Gianluca Sbardella ; Sabrina Castellano ; Caterina Vicidomini ; Dante Rotili ; Angela Nebbioso ; Marco Miceli ; Lucia Altucci ; Antonello Mai
- 关键词：Epigenetics ; Histone acetyltransferase modulators ; HAT ; Antitumor agents ; Anacardic acid
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：1 May 2008
- 卷：18
- 期：9
- 页码：2788-2792
- 文件大小：602 K
摘要
Pentadecylidenemalonate 1b, a simplified analogue of anacardic acid, was identified as the first mixed activator/inhibitor of histone acetyltransferases (HATs). It potentiates PCAF HAT activity while inhibiting those of p300/CBP and recombinant CBP. The remarkable apoptotic effect together with the ability to selectively acetylate histone versus non-histone substrates appoint 1b as a lead for the development of anticancer drugs.