Tra1 as a screening target for transcriptional activation domain discovery.

Bioorg Med Chem Lett 2009 Jul 18;19(14):3733-5. Epub 2009 May 18.

Department of Chemistry, University of Michigan, Ann Arbor, MI 48109, USA.

There is tremendous interest in developing activator artificial transcription factors that functionally mimic endogenous transcriptional activators for use as mechanistic probes, as components of synthetic cell circuitry, and in transcription-targeted therapies. Here, we demonstrate that a phage display selection against the transcriptional activation domain binding motif of the coactivator Tra1(TRRAP) produces distinct sequences that function with similar binding modes and potency as natural activators. These findings set the stage for binding screens with small molecule libraries against TAD binding motifs to yield next-generation small molecule TADs.

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http://dx.doi.org/10.1016/j.bmcl.2009.05.045DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4322765PMC
July 2009
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