Frizzled-7 receptor (FZD7)

Frizzled-7 receptor (FZD7) is a member of the Frizzled family of class F G protein-coupled receptors (GPCRs), characterized by a seven-transmembrane structure and a cysteine-rich extracellular domain. FZD7 functions as a primary cell-surface receptor for Wnt signaling proteins, playing crucial roles in embryonic development, regulation of stem and progenitor cells, and homeostasis of adult tissues. FZD7 is especially important in the migration of mesendodermal cells and is a key regulator in the renewal of intestinal stem cells. Overexpression and dysregulation of FZD7 are associated with tumorigenesis, particularly in gastrointestinal cancers such as colorectal cancer. Despite its strong validation as an oncology target, no approved drugs specifically modulate FZD7 in clinical practice, largely due to structural complexities and challenges in developing selective modulators. FZD7 signaling can proceed via Dishevelled (DVL)-dependent or G protein-coupled pathways depending on conformational state. Safety liabilities for therapeutic interventions include the risk of disrupting physiological functions of the Wnt-FZD7 axis in regenerative tissues.

Other names

Frizzled class receptor 7FZD7Fz-7FDZ7Frizzled-7Fz7

Modulation of Wnt signaling (via binding or blocking WNT ligands, or interfering with Dishevelled or G protein interactions)