title: New homogeneous high-throughput assays for inhibitors of β-catenin/Tcf protein-protein interactions.
abstract: The transcriptional activator β-catenin is the primary mediator of the canonical Wnt/β-catenin signaling pathway. The aberrant formation of the β-catenin/T-cell factor (Tcf) complex leads to many cancers and organ fibroses. Selective inhibition of β-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 β-catenin/Tcf interactions. These two new assays reproduce native β-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 β-catenin/Tcf protein-protein interactions.
authors.affiliation: Department of Chemistry, Center for Cell and Genome Science, University of Utah, Salt Lake City, UT 84112-0850, USA.
authors.forename: Min
authors.initials: M
authors.lastname: Zhang
authors.forename: Zheng
authors.initials: Z
authors.lastname: Huang
authors.forename: Binxun
authors.initials: B
authors.lastname: Yu
authors.forename: Haitao
authors.initials: H
authors.lastname: Ji
mesh_terms: D000595:Amino Acid Sequence; D001667:Binding, Competitive; D019921:Biotinylation; D005454:Fluorescence Polarization; D057166:High-Throughput Screening Assays / Q000379:methods*; D006801:Humans; D007700:Kinetics; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry / Q000378:metabolism; D011485:Protein Binding; D013194:Staining and Labeling; D051820:TCF Transcription Factors / Q000378:metabolism*; D013997:Time Factors; D051176:beta Catenin / Q000378:metabolism*
chemical_list: D010455:Peptides; D051820:TCF Transcription Factors; D051176:beta Catenin