Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 12, Pages 3690-3701Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.01.013
Keywords
Histone acetyltransferases modulators; p300/CBP; PCAF activator; KAT; Epigenetics
Funding
- Ministero dell'Universita e della Ricerca Scientifica e Tecnologica
- Fondazione Roma
- Universita di Salerno, Italy
- ATLAS [HEALTH-F4-2009-221952]
- Associazione Italiana per la Ricerca sul Cancro Funding Source: Custom
Ask authors/readers for more resources
A novel class of KAT modulators (long chain alkylidenemalonates, LoCAMs) has been identified. Variations of the alkyl chain length can change the activity profile from inhibition of both KAT3A/KAT2B (as derivative 2a) to the peculiar profile of pentadecylidenemalonate 1b, the first activator/inhibitor of histone acetyltransferases. Together with the powerful apoptotic effect (particularly notable if considering that anacardic acid and other KAT inhibitors are not cell permeable) appoint them as valuable biological tools to understand the mechanisms of lysine acetyltransferases. (C) 2011 Elsevier Ltd. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available
Share Paper
