Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs)

…, S Castellano, R Benedetti, A Tosco, C Ciliberti…

文献索引：Milite, Ciro; Castellano, Sabrina; Benedetti, Rosaria; Tosco, Alessandra; Ciliberti, Carmen; Vicidomini, Caterina; Boully, Ludovic; Franci, Gianluigi; Altucci, Lucia; Mai, Antonello; Sbardella, Gianluca Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 12 p. 3690 - 3701

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被引用次数: 21

摘要

A novel class of KAT modulators (long chain alkylidenemalonates, LoCAMs) has been identified. Variations of the alkyl chain length can change the activity profile from inhibition of both KAT3A/KAT2B (as derivative 2a) to the peculiar profile of pentadecylidenemalonate 1b, the first activator/inhibitor of histone acetyltransferases. Together with the powerful apoptotic effect (particularly notable if considering that anacardic acid and other KAT inhibitors are ...