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.

Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases / Gianluca, Sbardella; Sabrina, Castellano; Caterina, Vicidomini; Rotili, Dante; Angela, Nebbioso; Marco, Miceli; Lucia, Altucci; Mai, Antonello. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 18:9(2008), pp. 2788-2792. [10.1016/j.bmcl.2008.04.017]

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

ROTILI, Dante;MAI, Antonello
2008

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.
2008
anacardic acid; antitumor agents; epigenetics; hat; histone acetyltransferase modulators
01 Pubblicazione su rivista::01a Articolo in rivista
Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases / Gianluca, Sbardella; Sabrina, Castellano; Caterina, Vicidomini; Rotili, Dante; Angela, Nebbioso; Marco, Miceli; Lucia, Altucci; Mai, Antonello. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 18:9(2008), pp. 2788-2792. [10.1016/j.bmcl.2008.04.017]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/363940
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