Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 4, Pages 1132-1135Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.12.097
Keywords
Epigenetics; Chromatin remodeling; Histone acetyltransferase; 4-Hydroxyquinoline; Apoptosis; Cytodifferentiation; Histone acetylation; p300/CBP
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Funding
- PRIN
- FIRB [RBIP067F9E]
- RETI FIRB [RBPR05NWWC_006]
- European Union [200620, 200767]
- AIRC
- Regione Campania
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We identified a series of 4-hydroxyquinolines bearing a C1 to C15 alkyl chain at the C2 position and a carbethoxy/carboxy group at the C3 position of the quinoline nucleus (MC compounds), endowed with selective inhibitory activity against the p300/CBP HAT enzymes. Enzyme inhibition was investigated using in vitro HAT assays and by western blot analysis of cellular lysates to examine the acetylation levels of histone H3 and alpha-tubulin. When tested in U937 cells, some compounds displayed pro-apoptotic or cytodifferentiating properties. (C) 2009 Elsevier Ltd. All rights reserved.
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