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

N Mahindroo, C Punchihewa, AM Bail, N Fujii

Index: Mahindroo, Neeraj; Punchihewa, Chandanamali; Bail, Allison M.; Fujii, Naoaki Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 3 p. 946 - 949

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Citation Number: 15

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.