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

Bioorganic & Medicinal Chemistry Letters
Gianluca SbardellaAntonello Mai

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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Citations

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