Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylation
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HCT116 Cells
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Humans
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Lysine / analogs & derivatives*
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Lysine / chemical synthesis
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Lysine / chemistry*
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Lysine / pharmacology
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Niacinamide / pharmacology
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Recombinant Proteins / antagonists & inhibitors
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Recombinant Proteins / metabolism
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Sirtuins / antagonists & inhibitors*
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Sirtuins / metabolism
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Thioamides / chemical synthesis
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Thioamides / chemistry*
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Thioamides / pharmacology
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Tumor Suppressor Protein p53 / metabolism
Substances
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Recombinant Proteins
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Thioamides
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Tumor Suppressor Protein p53
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Niacinamide
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Sirtuins
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Lysine