Structural basis of Wnt recognition by Frizzled

Science. 2012 Jul 6;337(6090):59-64. doi: 10.1126/science.1222879. Epub 2012 May 31.

Abstract

Wnts are lipid-modified morphogens that play critical roles in development principally through engagement of Frizzled receptors. The 3.25 angstrom structure of Xenopus Wnt8 (XWnt8) in complex with mouse Frizzled-8 (Fz8) cysteine-rich domain (CRD) reveals an unusual two-domain Wnt structure, not obviously related to known protein folds, resembling a "hand" with "thumb" and "index" fingers extended to grasp the Fz8-CRD at two distinct binding sites. One site is dominated by a palmitoleic acid lipid group projecting from serine 187 at the tip of Wnt's thumb into a deep groove in the Fz8-CRD. In the second binding site, the conserved tip of Wnt's "index finger" forms hydrophobic amino acid contacts with a depression on the opposite side of the Fz8-CRD. The conservation of amino acids in both interfaces appears to facilitate ligand-receptor cross-reactivity, which has important implications for understanding Wnt's functional pleiotropy and for developing Wnt-based drugs for cancer and regenerative medicine.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acylation
  • Amino Acid Sequence
  • Animals
  • Binding Sites
  • Crystallography, X-Ray
  • Cysteine / chemistry
  • Fatty Acids, Monounsaturated / chemistry
  • Glycosylation
  • Hydrophobic and Hydrophilic Interactions
  • Ligands
  • Mice
  • Models, Molecular
  • Molecular Sequence Data
  • Protein Binding
  • Protein Folding
  • Protein Interaction Domains and Motifs
  • Protein Multimerization
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Receptors, G-Protein-Coupled / chemistry*
  • Receptors, G-Protein-Coupled / metabolism
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / metabolism
  • Wnt Proteins / chemistry*
  • Wnt Proteins / metabolism
  • Wnt Signaling Pathway
  • Xenopus Proteins / chemistry*
  • Xenopus Proteins / metabolism
  • Xenopus laevis

Substances

  • Fatty Acids, Monounsaturated
  • Ligands
  • Receptors, G-Protein-Coupled
  • Recombinant Proteins
  • Wnt Proteins
  • Xenopus Proteins
  • frizzled 8 protein, mouse
  • wnt8a protein, Xenopus
  • palmitoleic acid
  • Cysteine

Associated data

  • PDB/4F0A