Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases

G Sbardella, S Castellano, C Vicidomini, D Rotili…

文献索引：Sbardella, Gianluca; Castellano, Sabrina; Vicidomini, Caterina; Rotili, Dante; Nebbioso, Angela; Miceli, Marco; Altucci, Lucia; Mai, Antonello Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 9 p. 2788 - 2792

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被引用次数: 70

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.