Identification of a cell-active non-peptide sirtuin inhibitor containing N-thioacetyl lysine
| Autor: | Erika Imai, Hiroki Tsumoto, Tomomi Asaba, Takayoshi Suzuki, Hidehiko Nakagawa, Naoki Miyata |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
Niacinamide
SIRT3 Clinical Biochemistry Lysine Pharmaceutical Science Biochemistry Drug Discovery Humans Sirtuins Molecular Biology chemistry.chemical_classification biology Chemistry Organic Chemistry Acetylation HCT116 Cells Recombinant Proteins Thioamides Enzyme Enzyme inhibitor Cell culture Sirtuin biology.protein Molecular Medicine Histone deacetylase Tumor Suppressor Protein p53 |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 19:5670-5672 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2009.08.028 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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