Structural basis of the activation of c-MET receptor

Nat Commun. 2021 Jul 1;12(1):4074. doi: 10.1038/s41467-021-24367-3.

Abstract

The c-MET receptor is a receptor tyrosine kinase (RTK) that plays essential roles in normal cell development and motility. Aberrant activation of c-MET can lead to both tumors growth and metastatic progression of cancer cells. C-MET can be activated by either hepatocyte growth factor (HGF), or its natural isoform NK1. Here, we report the cryo-EM structures of c-MET/HGF and c-MET/NK1 complexes in the active state. The c-MET/HGF complex structure reveals that, by utilizing two distinct interfaces, one HGF molecule is sufficient to induce a specific dimerization mode of c-MET for receptor activation. The binding of heparin as well as a second HGF to the 2:1 c-MET:HGF complex further stabilize this active conformation. Distinct to HGF, NK1 forms a stable dimer, and bridges two c-METs in a symmetrical manner for activation. Collectively, our studies provide structural insights into the activation mechanisms of c-MET, and reveal how two isoforms of the same ligand use dramatically different mechanisms to activate the receptor.

Publication types

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

MeSH terms

  • Cell Line
  • Cryoelectron Microscopy
  • HEK293 Cells
  • Heparin / metabolism
  • Hepatocyte Growth Factor / chemistry*
  • Hepatocyte Growth Factor / metabolism*
  • Humans
  • Ligands
  • Models, Molecular
  • Protein Conformation
  • Protein Interaction Domains and Motifs
  • Protein Isoforms / metabolism
  • Proto-Oncogene Proteins c-met / chemistry*
  • Proto-Oncogene Proteins c-met / metabolism*
  • Receptors, Neurokinin-1 / metabolism

Substances

  • HGF protein, human
  • Ligands
  • Protein Isoforms
  • Receptors, Neurokinin-1
  • Hepatocyte Growth Factor
  • Heparin
  • MET protein, human
  • Proto-Oncogene Proteins c-met