Conformational changes at the agonist binding domain of the N-methyl-D-aspartic acid receptor

J Biol Chem. 2011 May 13;286(19):16953-7. doi: 10.1074/jbc.M111.224576. Epub 2011 Mar 24.

Abstract

The conformational changes in the agonist binding domain of the glycine-binding GluN1 and glutamate-binding GluN2A subunits of the N-methyl D-aspartic acid receptor upon binding agonists of varying efficacy have been investigated by luminescence resonance energy transfer (LRET) measurements. The LRET-based distances indicate a cleft closure conformational change at the GluN1 subunit upon binding agonists; however, no significant changes in the cleft closure are observed between partial and full agonists. This is consistent with the previously reported crystal structures for the isolated agonist binding domain of this receptor. Additionally, the LRET-based distances show that the agonist binding domain of the glutamate-binding GluN2A subunit exhibits a graded cleft closure with the extent of cleft closure being proportional to the extent of activation, indicating that the mechanism of activation in this subunit is similar to that of the glutamate binding α-amino-5-methyl-3-hydroxy-4-isoxazole propionate and kainate subtypes of the ionotropic glutamate receptors.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Crystallography, X-Ray / methods
  • Fluorescence Resonance Energy Transfer
  • Fluorescent Dyes / pharmacology
  • Hydrogen Bonding
  • Models, Molecular
  • Neurotransmitter Agents / chemistry
  • Patch-Clamp Techniques
  • Protein Binding
  • Protein Conformation
  • Receptors, Kainic Acid / chemistry
  • Receptors, N-Methyl-D-Aspartate / chemistry*
  • Xenopus laevis
  • alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid / chemistry

Substances

  • Fluorescent Dyes
  • Neurotransmitter Agents
  • Receptors, Kainic Acid
  • Receptors, N-Methyl-D-Aspartate
  • alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid