Inhibition of ErbB2(Her2) expression with small molecule transcription factor mimics.
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ABSTRACT:
SUBMITTER: Lee LW
PROVIDER: S-EPMC2782467 | biostudies-literature | 2009 Nov
REPOSITORIES: biostudies-literature
Publications
Inhibition of ErbB2(Her2) expression with small molecule transcription factor mimics.
Lee Lori W LW Taylor Christopher E C CE Desaulniers Jean-Paul JP Zhang Manchao M Højfeldt Jonas W JW Pan Quintin Q Mapp Anna K AK
Bioorganic & medicinal chemistry letters 20090901 21
Small molecules that mimic the transcriptional activation domain of eukaryotic transcriptional activators have the potential to serve as effective inhibitors of transcriptional processes. Here we show that one class of transcriptional activation domain mimics, amphipathic isoxazolidines, can be converted into inhibitors of gene expression mediated by the transcriptional activator ESX through small structural modifications. Addition of the small molecules leads to decreased expression of the cell ...[more]
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