Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 19, Pages 5670-5672Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.08.028
Keywords
Sirtuin inhibitor; Thioacetyl lysine; Non-peptide
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Funding
- Japan Society for the Promotion of Science
- Nagoya City University
- Ichihara International Scholarship Foundation
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To identify cell-active sirtuin inhibitors containing N-thioacetyl lysine, we synthesized compound 1, which was designed based on the structure of the reported N-ethoxycarbonylacetyl lysine-based sirtuin inhibitor NCS-12k. Compound 1 selectively inhibited SIRT1 in enzyme assays. Compound 1 also caused a dose-dependent increase in p53 acetylation in human colon cancer HCT116 cells, indicating the inhibition of SIRT1 in these cells. (C) 2009 Elsevier Ltd. All rights reserved.
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