1. Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs)
- Author
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Ciro Milite (a), Sabrina Castellano (a), Rosaria Benedetti (b, Alessandra Tosco (a), Carmen Ciliberti(a), Caterina Vicidomini (a), Ludovic Boully (a), Gianluigi Franci (b, Lucia Altucci (b, Antonello Mai (e), Gianluca Sbardella (a), Milite, C, Castellano, S, Benedetti, R, Tosco, A, Ciliberti, C, Vicidomini, C, Boully, L, Franci, G, Altucci, Lucia, Mai, A, and Sbardella, G.
- Subjects
Lysine Acetyltransferases ,Alkylation ,Blotting, Western ,Clinical Biochemistry ,Pharmaceutical Science ,Histone acetyltransferases modulators ,Biochemistry ,03 medical and health sciences ,0302 clinical medicine ,Cell Line, Tumor ,Drug Discovery ,Humans ,Epigenetics ,Enzyme Inhibitors ,Molecular Biology ,P300/CBP ,PCAF activator ,KAT ,Histone Acetyltransferases ,030304 developmental biology ,chemistry.chemical_classification ,0303 health sciences ,biology ,Activator (genetics) ,Organic Chemistry ,Biological activity ,U937 Cells ,Histone acetyltransferase ,Malonates ,Enzyme Activation ,Enzyme ,chemistry ,Acyltransferases ,030220 oncology & carcinogenesis ,biology.protein ,Molecular Medicine ,p300/CBP - 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. (C) 2011 Elsevier Ltd. All rights reserved.
- Published
- 2011
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