A locally closed conformation of a bacterial pentameric proton-gated ion channel

Nat Struct Mol Biol. 2012 May 13;19(6):642-9. doi: 10.1038/nsmb.2307.

Abstract

Pentameric ligand-gated ion channels mediate signal transduction through conformational transitions between closed-pore and open-pore states. To stabilize a closed conformation of GLIC, a bacterial proton-gated homolog from Gloeobacter violaceus whose open structure is known, we separately generated either four cross-links or two single mutations. We found all six mutants to be in the same 'locally closed' conformation using X-ray crystallography, sharing most of the features of the open form but showing a locally closed pore as a result of a concerted bending of all of its M2 helices. The mutants adopt several variant conformations of the M2-M3 loop, and in all cases an interacting lipid that is observed in the open form disappears. A single cross-linked mutant is functional, according to electrophysiology, and the locally closed structure of this mutant indicates that it has an increased flexibility. Further cross-linking, accessibility and molecular dynamics data suggest that the locally closed form is a functionally relevant conformation that occurs during allosteric gating transitions.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Allosteric Regulation
  • Amino Acid Sequence
  • Bacterial Proteins / chemistry*
  • Bacterial Proteins / genetics
  • Bacterial Proteins / metabolism
  • Crystallography, X-Ray
  • Cyanobacteria / chemistry*
  • Cyanobacteria / genetics
  • Cyanobacteria / metabolism
  • Cysteine / chemistry
  • Cysteine / genetics
  • Cysteine / metabolism
  • Ion Channel Gating
  • Ion Channels / chemistry*
  • Ion Channels / genetics
  • Ion Channels / metabolism
  • Molecular Dynamics Simulation
  • Mutation
  • Protein Conformation
  • Protons*

Substances

  • Bacterial Proteins
  • Ion Channels
  • Protons
  • Cysteine