Tra1 as a screening target for transcriptional activation domain discovery.

Abstract:

: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.

journal_name

Bioorg Med Chem Lett

authors

Majmudar CY,Labut AE,Mapp AK

doi

10.1016/j.bmcl.2009.05.045

subject

Has Abstract

pub_date

2009-07-15 00:00:00

pages

3733-5

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)00723-9

journal_volume

19

pub_type

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