Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 9, Pages 2788-2792Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.04.017
Keywords
epigenetics; histone acetyltransferase modulators; HAT; antitumor agents; anacardic acid
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Funding
- Associazione Italiana per la Ricerca sul Cancro Funding Source: Custom
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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. (c) 2008 Elsevier Ltd. All rights reserved.
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