title: Development of a novel fluorescence polarization-based assay for studying the β-catenin/Tcf4 interaction.
abstract: Aberrant activation of the Wnt/β-catenin signaling pathway is associated with a wide range of human cancers. The interaction of β-catenin with T cell factor (Tcf) is a key step in activation of proliferative genes in this pathway. Interruption of this interaction would be a valuable strategy as a tumor therapy. In this study, we developed a novel fluorescein isothiocyanate (FITC)-labeled Tcf4-derived probe for identification of inhibitors of the β-catenin/Tcf4 interaction using a fluorescence polarization assay. This assay shows high potential for use in high-throughput screening for the discovery of inhibitors of the β-catenin/Tcf4 interaction.
authors: Department of Pharmacology, State University of New York, Upstate Medical University, Syracuse, NY, USA.
authors: Wang
authors: W
authors: Tian
authors: Yan
authors: Y
authors: Xu
authors: Xiaofeng
authors: X
authors: Han
authors: Srinivas
authors: S
authors: Duggineni
authors: Xiaobing
authors: X
authors: Han
authors: Ziwei
authors: Z
authors: Huang
authors: Jing
authors: J
authors: An
mesh_terms: D051778:Basic Helix-Loop-Helix Leucine Zipper Transcription Factors / Q000378:metabolism*; D001667:Binding, Competitive / Q000187:drug effects; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005454:Fluorescence Polarization / Q000379:methods*; D057166:High-Throughput Screening Assays; D006801:Humans; D011485:Protein Binding / Q000187:drug effects; D054730:Protein Interaction Domains and Motifs / Q000187:drug effects; D000073940:Transcription Factor 4; D014157:Transcription Factors / Q000378:metabolism*; D051176:beta Catenin / Q000378:metabolism*
chemical_list: D051778:Basic Helix-Loop-Helix Leucine Zipper Transcription Factors; C532096:TCF4 protein, human; D000073940:Transcription Factor 4; D014157:Transcription Factors; D051176:beta Catenin