2. Academic Validation
  3. Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs)

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

  • Bioorg Med Chem. 2011 Jun 15;19(12):3690-701. doi: 10.1016/j.bmc.2011.01.013.
Ciro Milite 1,  Sabrina Castellano,  Rosaria Benedetti,  Alessandra Tosco,  Carmen Ciliberti,  Caterina Vicidomini,  Ludovic Boully,  Gianluigi Franci,  Lucia Altucci,  Antonello Mai,  Gianluca Sbardella
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy.
PMID: 21292492 DOI: 10.1016/j.bmc.2011.01.013
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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