Transcriptional up-regulation in cells mediated by a small molecule

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

Research output: Contribution to journalArticle

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 languageEnglish (US)
Pages (from-to)10654-10655
Number of pages2
JournalJournal of the American Chemical Society
Volume129
Issue number35
DOIs
StatePublished - Sep 5 2007
Externally publishedYes

Fingerprint

Activator Appliances
Up-Regulation
Molecules
Transcription
Transcription Factors
Transcription factors
DNA
Genes
Cells
Therapeutics

ASJC Scopus subject areas

  • Chemistry(all)

Cite this

Transcriptional up-regulation in cells mediated by a small molecule. / Rowe, Steven; Casey, Ryan J.; Brennan, Brian B.; Buhrlage, Sara J.; Mapp, Anna K.

In: Journal of the American Chemical Society, Vol. 129, No. 35, 05.09.2007, p. 10654-10655.

Research output: Contribution to journalArticle

Rowe, Steven ; Casey, Ryan J. ; Brennan, Brian B. ; Buhrlage, Sara J. ; Mapp, Anna K. / Transcriptional up-regulation in cells mediated by a small molecule. In: Journal of the American Chemical Society. 2007 ; Vol. 129, No. 35. pp. 10654-10655.
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