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1.
Indole-2-amide based biochemical antagonist of Dishevelled PDZ domain interaction down-regulates Dishevelled-driven Tcf transcriptional activity.
Mahindroo, Neeraj; Punchihewa, Chandanamali; Bail, Allison M; Fujii, Naoaki.
Bioorg Med Chem Lett ; 18(3): 946-9, 2008 Feb 01.
Article in English | MEDLINE | ID: mdl-18180158

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.


Subject(s)
Adaptor Proteins, Signal Transducing/antagonists & inhibitors , Amides/chemical synthesis , Amides/pharmacology , Indoles/chemical synthesis , Indoles/pharmacology , Models, Molecular , Phosphoproteins/antagonists & inhibitors , TCF Transcription Factors/metabolism , Adaptor Proteins, Signal Transducing/metabolism , Amides/chemistry , Apoptosis/drug effects , Combinatorial Chemistry Techniques , Dishevelled Proteins , Humans , Indoles/chemistry , Molecular Structure , PDZ Domains/drug effects , Phosphoproteins/metabolism , Structure-Activity Relationship , TCF Transcription Factors/drug effects , Transcription, Genetic/drug effects , Wnt Proteins/physiology
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