Revisiting channel allostery: a coherent mechanism in IP₃ and ryanodine receptors

Sci Signal. 2012 May 22;5(225):pe24. doi: 10.1126/scisignal.2003148.

Abstract

The inositol 1,4,5-trisphosphate (IP₃) receptor is an IP₃-gated calcium ion (Ca²⁺) channel that mediates intracellular IP₃-Ca²⁺ signaling. A fundamental question--how IP₃ gates the Ca²⁺ channel within the IP₃ receptor--remains unanswered. A new crystal structure of the N-terminal region of the IP₃ receptor reveals allosteric changes by ligand binding and its similarity to the corresponding region of ryanodine receptor. Docking of the crystal structures in the electron microscopy map and an IP₃ receptor-ryanodine receptor chimera consistently supported a coherent gating mechanism in these receptors. An intriguing feature was the long distance between the IP₃-binding sites and the Ca²⁺ channel, suggesting that long-range allosteric coupling occurs between these regions upon gating of the channel. These results help integrate previous knowledge on the IP₃ and ryanodine receptors and also provide a new framework for understanding the gating mechanism.

MeSH terms

  • Allosteric Regulation
  • Animals
  • Calcium Signaling / physiology*
  • Cryoelectron Microscopy
  • Crystallography, X-Ray
  • Fluorescence Resonance Energy Transfer
  • Humans
  • Inositol 1,4,5-Trisphosphate Receptors / chemistry*
  • Inositol 1,4,5-Trisphosphate Receptors / ultrastructure
  • Ion Channel Gating / physiology*
  • Models, Molecular
  • Peptide Fragments / chemistry
  • Protein Conformation
  • Protein Structure, Tertiary
  • Ryanodine Receptor Calcium Release Channel / chemistry*
  • Ryanodine Receptor Calcium Release Channel / ultrastructure
  • Structure-Activity Relationship

Substances

  • Inositol 1,4,5-Trisphosphate Receptors
  • Peptide Fragments
  • Ryanodine Receptor Calcium Release Channel