New homogeneous high-throughput assays for inhibitors of beta-catenin/Tcf protein-protein interactions

作者：Zhang Min; Huang Zheng; Yu Binxun; Ji Haitao^*

来源：Analytical Biochemistry, 2012, 424(1): 57-63.

DOI：10.1016/j.ab.2012.02.018

• High-throughput screening
• AlphaScreen
• Fluorescence polarization
• beta-Catenin/Tcf interactions
• Wnt signaling

The transcriptional activator p-catenin is the primary mediator of the canonical Wnt/beta-catenin signaling pathway. The aberrant formation of the beta-catenin/T-cell factor (Tcf) complex leads to many cancers and organ fibroses. Selective inhibition of beta-catenin/Tcf protein-protein interactions represents an appealing therapeutic strategy. In this study, two new robust, homogeneous high-throughput assays, AlphaScreen and fluorescence polarization, were established to study beta-catenin/Tcf interactions. These two new assays reproduce native beta-catenin/Tcf interactions, quantify inhibitory potency, and are complementary with each other. The establishment of these two high-throughput screenings enables quick identification of inhibitors of beta-catenin/Tcf protein-protein interactions.

• 出版日期2012-5-1