Journal
CANCER CELL
Volume 13, Issue 5, Pages 454-463Publisher
CELL PRESS
DOI: 10.1016/j.ccr.2008.03.004
Keywords
-
Categories
Funding
- Cancer Research UK [A6613] Funding Source: Medline
- Medical Research Council Funding Source: Medline
Ask authors/readers for more resources
We have carried out a cell-based screen aimed at discovering small molecules that activate p53 and have the potential to decrease tumor growth. Here, we describe one of our hit compounds, tenovin-1, along with a more water-soluble analog, tenovin-6. Via a yeast genetic screen, biochemical assays, and target validation studies in mammalian cells, we show that tenovins act through inhibition of the protein-deacetylating activities of SirT1 and SirT2, two important members of the sirtuin family. Tenovins are active on mammalian cells at one-digit micromolar concentrations and decrease tumor growth in vivo as single agents. This underscores the utility of these compounds as biological tools for the study of sirtuin function as well as their potential therapeutic interest.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available