Frizzled-1 receptor (FZD1)

Frizzled-1 receptor is a member of the Frizzled family of G protein-coupled receptors (GPCRs), encoded by the FZD1 gene in humans. It contains a conserved extracellular cysteine-rich domain (CRD) necessary for binding lipid-modified Wnt ligands, seven transmembrane domains, and signals primarily by activating canonical Wnt/β-catenin as well as non-canonical PCP pathways. FZD1 is expressed in diverse tissues, including the central nervous system where it is present in dopamine transporter-positive neurons. Functionally, it regulates cell fate, proliferation, differentiation, and polarity during development and in adult tissue. Aberrant FZD1 or Wnt signaling is implicated in cancers, neurodegenerative diseases, and developmental disorders. The receptor can be modulated at multiple points by endogenous antagonists (such as sFRPs and DKK proteins) and potentially by pharmacological agents targeting downstream Wnt signaling. There are currently no approved drugs that specifically and selectively target Frizzled-1 receptor.

Other names

Frizzled-1Fz-1FZD1

Modulation of Wnt/β-catenin signaling by agonism or antagonism of the receptor-ligand interaction - Inhibition of receptor activity by sFRPs (secreted Frizzled-related proteins), which can bind Wnt ligands or the receptor CRD to block signaling