Frizzled-1 receptor, Frizzled-2 receptor, Frizzled-7 receptor (FZD1, FZD2, FZD7)

Frizzled-1, Frizzled-2, and Frizzled-7 receptors are integral membrane proteins belonging to the Frizzled family of atypical class F G protein-coupled receptors, notable for their signature seven-transmembrane domains and conserved extracellular cysteine-rich domain. They primarily serve as cell-surface receptors for secreted Wnt ligands, orchestrating signal transduction across canonical (Wnt/β-catenin), planar cell polarity, and Wnt/Ca²⁺ pathways. These receptors play fundamental roles in embryonic development, cell fate, polarity, and proliferation, and are centrally involved in tumorigenesis (particularly gastrointestinal and melanoma) and other diseases. FZD7, in particular, is linked to intestinal stem cell renewal and gastrointestinal cancers. Major therapeutic approaches in development involve targeting these receptors with antibodies or decoy proteins to inhibit pro-tumorigenic Wnt/FZD signaling, but clinical application is limited by potential stem cell and tissue homeostasis toxicity.

Other names

FZD1: Frizzled homolog 1FZD1: Fz-1FZD2: Frizzled homolog 2FZD2: Fz-2FZD7: Frizzled homolog 7FZD7: Fz-7Common family alias: Frizzled receptorCommon family alias: FZD receptorCommon family alias: Fz receptor

Antagonists/inhibitors: Block Wnt ligand binding, disrupt Wnt/β-catenin (canonical) or non-canonical signal transduction, leading to reduced cell proliferation and increased apoptosis in cancer models. Decoy receptors: Sequester Wnt ligands to prevent activation of cell-surface FZD receptors