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Frizzled family receptors (FZD) are a group of G protein-coupled receptors that serve as the primary cell surface receptors for Wnt glycoproteins[2][4][7]. Frizzled proteins (ten homologs in humans, FZD1–FZD10) possess seven transmembrane domains and are integral to both canonical (Wnt/β-catenin) and non-canonical Wnt signaling pathways[2][4][10]. Upon Wnt ligand binding, Frizzled receptors often heterodimerize with co-receptors LRP5 or LRP6, leading to signal transduction cascades that regulate gene transcription, cell fate, embryonic patterning, tissue regeneration, and stem cell maintenance[2][4][5][6]. Dysregulation of Wnt/Frizzled signaling is implicated in diverse diseases, especially cancer, bone disorders, and fibrosis[4][5]. Several experimental drugs target Frizzled-mediated signaling, but safety concerns remain significant due to the pathway's essential physiological roles in adult tissue homeostasis[4][6].
Antagonist antibody blocks ligand binding to Frizzled, preventing downstream Wnt signal transduction. Decoy receptor competition for Wnt ligand. Inhibition of Wnt ligand secretion (upstream shutdown of receptor activation).
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