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Updated: Jul 5, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases
Gianluca Sbardella1, Sabrina Castellano, Caterina Vicidomini
1Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy. gsbardella@unisa.it
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.
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