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. (C) 2011 Elsevier Ltd. All rights reserved.

*** IBB - CNR ***

Dipartimento di Scienze Farmaceutiche, Università Degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy

Dipartimento di Patologia Generale, Seconda Università Degli Studi di Napoli, Vico L. De Crecchio 7, 80138 Napoli, Italy

Dipartimento di Fisica, Università di Napoli Federico II, Napoli, Italy

IGB-CNR, Via Pietro Castellino, 80100, Napoli, Italy

Dipartimento di Chimica e Tecnologie Del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, Sapienza Università di Roma, P.le A. Moro 5, 00185 Roma, Italy

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