Abstract

Bicyclic peptidomimetics bind the transcriptional coactivator β-catenin. A structure-based design strategy has been applied to minimize a 52 amino acid binding motif into bicyclic 16-mer β-sheet mimetics. The biologically most active mimetic exhibits robust cellular uptake and inhibits Wnt signaling in a cell-based assay, as reported by Tom N. Grossmann and co-workers in their Research Article on page 13937.

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