Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases

Gianluca Sbardella
Sabrina Castellano
Caterina Vicidomini
Dante Rotili
Angela Nebbioso
Marco Miceli
Lucia Altucci
Antonello Mai

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Publication date

January 2008

DOI

10.1016/j.bmcl.2008.04.017

Publisher

Elsevier BV

Abstract

Pentadecylidenemalonate 1b, a simplified analogue of anacardic acid, was identified as the first mixed activator/inhibitor of histone acetyltransferases (HATs). It potentiates PCAF HAT activity while inhibiting those of p300/CBP and recombinant CBP. The remarkable apoptotic effect together with the ability to selectively acetylate histone versus non-histone substrates appoint 1b as a lead for the development of anticancer drugs. © 2008 Elsevier Ltd. All rights reserved

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Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases

Abstract

Extracted data

Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases

Abstract

Extracted data

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