A novel histone deacetylase inhibitor identified by high-throughput transcriptional screening of a compound library

Gloria H. Su, Taylor A. Sohn, Byungwoo Ryu, Scott E. Kern

    Research output: Contribution to journalArticle

    185 Scopus citations

    Abstract

    Libraries of compounds are increasingly becoming commercially available for the use of individual academic laboratories. A high-throughput system based on a stably integrated transcriptional reporter was used to screen a library of random compounds to identify agents that conferred robust augmentation of a signal transduction pathway. A novel histone deacetylase (HDAC) inhibitor, termed scriptaid, conferred the greatest effect, a 12- to 18-fold augmentation. This facilitation of transcriptional events was generally applicable to exogenous gene constructs, including vital and cellular promoters, different cell lines and reporter genes, and stably integrated and transiently introduced sequences. Scriptaid did not interfere with a further induction provided by stimulation of the cognate signal transduction pathway (transforming growth factor β/Smad4), which implied the functional independence of ligand-stimulated transcriptional activation and histone acetylation states in this system. Additional insights into this and other signal transduction systems are likely to be afforded through the application of compound screening technologies.

    Original languageEnglish (US)
    Pages (from-to)3137-3142
    Number of pages6
    JournalCancer Research
    Volume60
    Issue number12
    StatePublished - Jun 15 2000

    ASJC Scopus subject areas

    • Oncology
    • Cancer Research

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