Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs) |
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| Authors: | Milite Ciro Castellano Sabrina Benedetti Rosaria Tosco Alessandra Ciliberti Carmen Vicidomini Caterina Boully Ludovic Franci Gianluigi Altucci Lucia Mai Antonello Sbardella Gianluca |
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| Affiliation: | Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy. |
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| Abstract: | 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 not cell permeable) appoint them as valuable biological tools to understand the mechanisms of lysine acetyltransferases. |
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