Transcriptional up-regulation in cells mediated by a small molecule

Steven P. Rowe, Ryan J. Casey, Brian B. Brennan, Sara J. Buhrlage, Anna K. Mapp

Research output: Contribution to journalArticlepeer-review


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 languageEnglish (US)
Pages (from-to)10654-10655
Number of pages2
JournalJournal of the American Chemical Society
Issue number35
StatePublished - Sep 5 2007
Externally publishedYes

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)
  • Biochemistry
  • Colloid and Surface Chemistry


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