Candidate amino acids involved in H+ gating of acid-sensing ion channel 1a

J Biol Chem. 2008 Jan 4;283(1):572-581. doi: 10.1074/jbc.M706811200. Epub 2007 Nov 1.

Abstract

Acid-sensing ion channels are ligand-gated cation channels, gated by extracellular H(+). H(+) is the simplest ligand possible, and whereas for larger ligands that gate ion channels complex binding sites in the three-dimensional structure of the proteins have to be assumed, H(+) could in principle gate a channel by titration of a single amino acid. Experimental evidence suggests a more complex situation, however. For example, it has been shown that extracellular Ca(2+) ions compete with H(+); probably Ca(2+) ions bound to the extracellular loop of ASICs stabilize the closed state of the channel and have to be displaced before the channel can open. In such a scheme, amino acids contributing to Ca(2+) binding would also be candidates contributing to H(+) gating. In this study we systematically screened more than 40 conserved, charged amino acids in the extracellular region of ASIC1a for a possible contribution to H(+) gating. We identified four amino acids where substitution strongly affects H(+) gating: Glu(63), His(72)/His(73), and Asp(78). These amino acids are highly conserved among H(+)-sensitive ASICs and are candidates for the "H(+) sensor" of ASICs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acid Sensing Ion Channels
  • Amino Acid Sequence
  • Amino Acid Substitution
  • Amino Acids / genetics*
  • Amino Acids / metabolism
  • Animals
  • Aspartic Acid / genetics
  • Aspartic Acid / metabolism
  • Binding Sites / genetics
  • Calcium / metabolism
  • Female
  • Glutamic Acid / genetics
  • Glutamic Acid / metabolism
  • Histidine / genetics
  • Histidine / metabolism
  • Hydrogen-Ion Concentration
  • Ion Channel Gating / genetics*
  • Ion Channel Gating / physiology
  • Membrane Proteins / genetics*
  • Membrane Proteins / metabolism
  • Membrane Proteins / physiology
  • Models, Molecular
  • Molecular Sequence Data
  • Nerve Tissue Proteins / genetics*
  • Nerve Tissue Proteins / metabolism
  • Nerve Tissue Proteins / physiology
  • Oocytes / metabolism
  • Protein Binding
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Rats
  • Sequence Homology, Amino Acid
  • Sodium Channels / genetics*
  • Sodium Channels / metabolism
  • Sodium Channels / physiology
  • Structure-Activity Relationship
  • Xenopus laevis

Substances

  • Acid Sensing Ion Channels
  • Amino Acids
  • Membrane Proteins
  • Nerve Tissue Proteins
  • Sodium Channels
  • Aspartic Acid
  • Glutamic Acid
  • Histidine
  • Calcium