Crystal structures of the extracellular domain of LRP6 and its complex with DKK1

Nat Struct Mol Biol. 2011 Oct 9;18(11):1204-10. doi: 10.1038/nsmb.2139.

Abstract

Low-density-lipoprotein (LDL) receptor-related proteins 5 and 6 (LRP5/6) are Wnt co-receptors essential for Wnt/β-catenin signaling. Dickkopf 1 (DKK1) inhibits Wnt signaling by interacting with the extracellular domains of LRP5/6 and is a drug target for multiple diseases. Here we present the crystal structures of a human LRP6-E3E4-DKK1 complex and the first and second halves of human LRP6's four propeller-epidermal growth factor (EGF) pairs (LRP6-E1E2 and LRP6-E3E4). Combined with EM analysis, these data demonstrate that LRP6-E1E2 and LRP6-E3E4 form two rigid structural blocks, with a short intervening hinge that restrains their relative orientation. The C-terminal domain of DKK1 (DKK1c) interacts with the top surface of the LRP6-E3 YWTD propeller and given their structural similarity, probably also that of the LRP6-E1 propeller, through conserved hydrophobic patches buttressed by a network of salt bridges and hydrogen bonds. Our work provides key insights for understanding LRP5/6 structure and the interaction of LRP5/6 with DKK, as well as for drug discovery.

Publication types

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

MeSH terms

  • Crystallography, X-Ray
  • Epidermal Growth Factor / chemistry
  • Epidermal Growth Factor / genetics
  • Epidermal Growth Factor / metabolism
  • Humans
  • Intercellular Signaling Peptides and Proteins / chemistry*
  • Intercellular Signaling Peptides and Proteins / metabolism
  • Low Density Lipoprotein Receptor-Related Protein-6 / chemistry*
  • Low Density Lipoprotein Receptor-Related Protein-6 / metabolism
  • Models, Molecular
  • Molecular Sequence Data
  • Multiprotein Complexes
  • Protein Structure, Tertiary*
  • Signal Transduction / physiology

Substances

  • DKK1 protein, human
  • Intercellular Signaling Peptides and Proteins
  • Low Density Lipoprotein Receptor-Related Protein-6
  • Multiprotein Complexes
  • Epidermal Growth Factor

Associated data

  • PDB/3S8V
  • PDB/3S8Z
  • PDB/3S94