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

Bioorganic & Medicinal Chemistry Letters
Neeraj MahindrooNaoaki Fujii

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.

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Citations

Mar 3, 2009·Nature Chemical Biology·Yingnan ZhangSachdev S Sidhu
Mar 14, 2012·Proceedings of the National Academy of Sciences of the United States of America·Daniele V F TaurielloMadelon M Maurice
Dec 18, 2009·Colorectal Disease : the Official Journal of the Association of Coloproctology of Great Britain and Ireland·S L McDonald, A R Silver
Apr 22, 2020·Advanced Therapeutics·Nikolaj R ChristensenKristian Strømgaard
Jul 13, 2021·Drug Discovery Today·Avradip ChatterjeeManash K Paul

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