Abstract
Activator artificial transcription factors, molecules that seek out specific genes and up-regulate their transcription, are desirable as mechanistic tools and as potential therapeutic agents. One challenge has been the identification of small molecule-based activator ATFs that function in cellular systems. Here we demonstrate that an amphipathic isoxazolidine activates transcription up to 80-fold in human cells when targeted to a specific promoter. Analogous to natural transcriptional activators, the function of the isoxazolidine appears to be independent of the DNA-targeting moiety, suggesting that the molecule will be effective in a variety of contexts. This is thus a critical step toward activator ATFs constructed from small molecule components.
Original language | English (US) |
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Pages (from-to) | 10654-10655 |
Number of pages | 2 |
Journal | Journal of the American Chemical Society |
Volume | 129 |
Issue number | 35 |
DOIs | |
State | Published - Sep 5 2007 |
Externally published | Yes |
ASJC Scopus subject areas
- Catalysis
- General Chemistry
- Biochemistry
- Colloid and Surface Chemistry