Chemical rescue of histidine selectivity filter mutants of the M2 ion channel of influenza A virus

J Biol Chem. 2005 Jun 3;280(22):21463-72. doi: 10.1074/jbc.M412406200. Epub 2005 Mar 22.

Abstract

The influenza virus M2 proton-selective ion channel activity facilitates virus uncoating, a process that occurs in the acidic environment of the endosome. The M2 channel causes acidification of the interior of the virus particle, which results in viral protein-protein dissociation. The M2 protein is a homotetramer that contains in its aqueous pore a histidine residue (His-37) that acts as a selectivity filter and a tryptophan residue (Trp-41) that acts as a channel gate. Substitution of His-37 modifies M2 ion channel properties drastically. However, the results of such experiments are difficult to interpret because substitution of His-37 could cause gross structural changes to the channel pore. We described here experiments in which partial or, in some cases, full rescue of specific M2 ion channel properties of His-37 substitution mutants was achieved by addition of imidazole to the bathing medium. Chemical rescue was demonstrated for three histidine substitution mutant ion channels (M2-H37G, M2-H37S, and M2-H37T) and for two double mutants in which the Trp-41 channel gate was also mutated (H37G/W41Y and H37G/W41A). Currents of the M2-H37G mutant ion channel were inhibited by Cu(II), which has been shown to coordinate with His-37 in the wild-type channel. Chemical rescue was very specific for imidazole. Buffer molecules that were neutral when protonated (4-morpholineethanesulfonic acid and 3-morpholino-2-hydroxypropanesulfonic acid) did not rescue ion channel activity of the M2-H37G mutant ion channel, but 1-methylimidazole did provide partial rescue of function. These results were consistent with a model for proton transport through the pore of the wild-type channel in which the imidazole side chain of His-37 acted as an intermediate proton acceptor/donor group.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Alkanesulfonic Acids / pharmacology
  • Amantadine / pharmacology
  • Animals
  • Buffers
  • Cell Membrane / metabolism
  • Copper / chemistry
  • Dose-Response Relationship, Drug
  • Endosomes
  • Genotype
  • Histidine / chemistry*
  • Hydrogen-Ion Concentration
  • Imidazoles / chemistry
  • Imidazoles / pharmacology
  • Ions
  • Kinetics
  • Microscopy, Fluorescence
  • Models, Biological
  • Models, Chemical
  • Morpholines / pharmacology
  • Mutation*
  • Oocytes / metabolism
  • Polymerase Chain Reaction
  • Protein Binding
  • Protons
  • RNA, Messenger / metabolism
  • Sulfonic Acids / pharmacology
  • Time Factors
  • Tryptophan / chemistry
  • Viral Matrix Proteins / genetics*
  • Viral Matrix Proteins / metabolism
  • Xenopus laevis

Substances

  • 3-morpholino-2-hydroxypropanesulfonic acid
  • Alkanesulfonic Acids
  • Buffers
  • Imidazoles
  • Ions
  • M2 protein, Influenza A virus
  • Morpholines
  • Protons
  • RNA, Messenger
  • Sulfonic Acids
  • Viral Matrix Proteins
  • 2-(N-morpholino)ethanesulfonic acid
  • Histidine
  • Copper
  • imidazole
  • Tryptophan
  • Amantadine