Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 23, Pages 8158-8166Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.10.022
Keywords
Histone methyltransferase; Small molecule inhibitor; Bisubstrate inhibitor; Epigenetics; SET7/9
Funding
- Ministry of Education, Science, Sports and Culture, Japan [19201044, 19790090, 22790106]
- Mochida Memorial Foundation
- Astellas Foundation
- Grants-in-Aid for Scientific Research [22790106, 19201044, 19790090] Funding Source: KAKEN
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Histone modification, for example, by histone deacetylase (HDAC) and histone lysine methyltransferase (HMT), plays an important role in regulating gene expression. To obtain novel inhibitors as tools for investigating the physiological function of members of the HMT family, we designed and synthesized novel inhibitors, which are amine analogues of adenosylmethionine (AdoMet; the cofactor utilized in the methylation reaction) bearing various alkylamino groups coupled via an ethylene linker. The inhibitory activities of these compounds towards SET7/9, an HMT, were evaluated. It was found that introduction of an alkylamino group increased the inhibitory activity. (C) 2010 Elsevier Ltd. All rights reserved.
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