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An allosteric ligand of Frizzled4
Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis. Wnt proteins initiate cell signaling by binding Frizzled (Fz) receptors, a family of G protein-coupled receptors. FzM1 is an allosteric ligand of Fz4. At 10 µM, it inhibits nuclear translocation of β-catenin in U87MG glioma cells treated with lithium chloride, a GSK3 inhibitor that enhances the Wnt canonical signaling pathway. FzM1 impairs the ability of U87MG cells to form neurospheres in culture and stimulates the differentiation of Caco-2 epithelial colorectal adenocarcinoma cells.
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