Design of triazole-stapled BCL9 α-helical peptides to target the β-catenin/B-cell CLL/lymphoma 9 (BCL9) protein–protein interaction

SA Kawamoto, A Coleska, X Ran, H Yi…

Index: Kawamoto, Steven A.; Coleska, Adriana; Ran, Xu; Yi, Han; Yang, Chao-Yie; Wang, Shaomeng Journal of Medicinal Chemistry, 2012 , vol. 55, # 3 p. 1137 - 1146

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Citation Number: 102

Abstract

The interaction between β-catenin and B-cell CLL/lymphoma 9 (BCL9), critical for the transcriptional activity of β-catenin, is mediated by a helical segment from BCL9 and a large binding groove in β-catenin. Design of potent, metabolically stable BCL9 peptides represents an attractive approach to inhibit the activity of β-catenin. In this study, we report the use of the Huisgen 1, 3-dipolar cycloaddition reaction to generate triazole-stapled ...