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Bioorg Med Chem Lett. 2008 Feb 1;18(3):946-9. doi: 10.1016/j.bmcl.2007.12.039. Epub 2007 Dec 23.

Indole-2-amide based biochemical antagonist of Dishevelled PDZ domain interaction down-regulates Dishevelled-driven Tcf transcriptional activity.

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1
Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, TN 38105, USA.

Abstract

We designed and synthesized a series of indole-2-amide-based compounds that antagonize interaction between the Dishevelled (Dvl) PDZ domain and a peptide derived from the natural PDZ ligand Frizzled-7 (Fz7). These compounds inhibit Tcf-mediated transcription activated by exogenous Dvl via the biochemical antagonism. We confirmed tumor cell-selective activation of caspases by these compounds.

PMID:
18180158
DOI:
10.1016/j.bmcl.2007.12.039
[Indexed for MEDLINE]
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