title: Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs).
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.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy.
authors.forename: Ciro
authors.initials: C
authors.lastname: Milite
authors.forename: Sabrina
authors.initials: S
authors.lastname: Castellano
authors.forename: Rosaria
authors.initials: R
authors.lastname: Benedetti
authors.forename: Alessandra
authors.initials: A
authors.lastname: Tosco
authors.forename: Carmen
authors.initials: C
authors.lastname: Ciliberti
authors.forename: Caterina
authors.initials: C
authors.lastname: Vicidomini
authors.forename: Ludovic
authors.initials: L
authors.lastname: Boully
authors.forename: Gianluigi
authors.initials: G
authors.lastname: Franci
authors.forename: Lucia
authors.initials: L
authors.lastname: Altucci
authors.forename: Antonello
authors.initials: A
authors.lastname: Mai
authors.forename: Gianluca
authors.initials: G
authors.lastname: Sbardella
mesh_terms: D000478:Alkylation / Q000187:drug effects; D015153:Blotting, Western; D045744:Cell Line, Tumor; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051548:Histone Acetyltransferases / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D008314:Malonates / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D020298:U937 Cells
chemical_list: D004791:Enzyme Inhibitors; D008314:Malonates; D051548:Histone Acetyltransferases