Argos inhibits epidermal growth factor receptor signalling by ligand sequestration

Nature. 2004 Aug 26;430(7003):1040-4. doi: 10.1038/nature02840.

Abstract

The epidermal growth factor receptor (EGFR) has critical functions in development and in many human cancers. During development, the spatial extent of EGFR signalling is regulated by feedback loops comprising both well-understood activators and less well-characterized inhibitors. In Drosophila melanogaster the secreted protein Argos functions as the only known extracellular inhibitor of EGFR, with clearly identified roles in multiple stages of development. Argos is only expressed when the Drosophila EGFR (DER) is activated at high levels, and downregulates further DER signalling. Although there is ample genetic evidence that Argos inhibits DER activation, the biochemical mechanism has not been established. Here we show that Argos inhibits DER signalling without interacting directly with the receptor, but instead by sequestering the DER-activating ligand Spitz. Argos binds tightly to the EGF motif of Spitz and forms a 1:1 (Spitz:Argos) complex that does not bind DER in vitro or at the cell surface. Our results provide an insight into the mechanism of Argos function, and suggest new strategies for EGFR inhibitor design.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Binding Sites
  • Down-Regulation
  • Drosophila Proteins / antagonists & inhibitors*
  • Drosophila Proteins / metabolism*
  • Drosophila melanogaster / metabolism*
  • Electron Spin Resonance Spectroscopy
  • Epidermal Growth Factor / antagonists & inhibitors
  • Epidermal Growth Factor / metabolism*
  • ErbB Receptors / antagonists & inhibitors*
  • ErbB Receptors / metabolism*
  • Eye Proteins / metabolism*
  • Ligands
  • Membrane Proteins / antagonists & inhibitors
  • Membrane Proteins / metabolism*
  • Nerve Tissue Proteins / metabolism*
  • Protein Binding
  • Protein Kinase Inhibitors*
  • Protein Kinases / metabolism*
  • Receptors, Invertebrate Peptide / antagonists & inhibitors*
  • Receptors, Invertebrate Peptide / metabolism*
  • Signal Transduction*

Substances

  • Drosophila Proteins
  • Eye Proteins
  • Ligands
  • Membrane Proteins
  • Nerve Tissue Proteins
  • Protein Kinase Inhibitors
  • Receptors, Invertebrate Peptide
  • aos protein, Drosophila
  • spi protein, Drosophila
  • Epidermal Growth Factor
  • Protein Kinases
  • Egfr protein, Drosophila
  • ErbB Receptors