Structural insights into the activation of metabotropic glutamate receptors

Nature. 2019 Feb;566(7742):79-84. doi: 10.1038/s41586-019-0881-4. Epub 2019 Jan 23.

Abstract

Metabotropic glutamate receptors are family C G-protein-coupled receptors. They form obligate dimers and possess extracellular ligand-binding Venus flytrap domains, which are linked by cysteine-rich domains to their 7-transmembrane domains. Spectroscopic studies show that signalling is a dynamic process, in which large-scale conformational changes underlie the transmission of signals from the extracellular Venus flytraps to the G protein-coupling domains-the 7-transmembrane domains-in the membrane. Here, using a combination of X-ray crystallography, cryo-electron microscopy and signalling studies, we present a structural framework for the activation mechanism of metabotropic glutamate receptor subtype 5. Our results show that agonist binding at the Venus flytraps leads to a compaction of the intersubunit dimer interface, thereby bringing the cysteine-rich domains into close proximity. Interactions between the cysteine-rich domains and the second extracellular loops of the receptor enable the rigid-body repositioning of the 7-transmembrane domains, which come into contact with each other to initiate signalling.

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

  • Allosteric Regulation
  • Cryoelectron Microscopy
  • Crystallography, X-Ray
  • Cysteine / chemistry
  • Cysteine / metabolism
  • Humans
  • Ligands
  • Models, Molecular
  • Protein Domains
  • Protein Stability
  • Receptor, Metabotropic Glutamate 5 / chemistry*
  • Receptor, Metabotropic Glutamate 5 / metabolism*
  • Receptor, Metabotropic Glutamate 5 / ultrastructure
  • Signal Transduction*

Substances

  • GRM5 protein, human
  • Ligands
  • Receptor, Metabotropic Glutamate 5
  • Cysteine