Interactions between a pore-blocking peptide and the voltage sensor of the sodium channel: an electrostatic approach to channel geometry

Neuron. 1996 Feb;16(2):407-13. doi: 10.1016/s0896-6273(00)80058-6.

Abstract

Few experimental data illuminate the relationship between the molecular structures that mediate ion conduction through voltage-dependent ion channels and the structures responsible for sensing transmembrane voltage and controlling gating. To fill this void, we have used a strongly cationic, mutated mu-conotoxin peptide, which only partially blocks current through voltage-dependent sodium channels, to study voltage-dependent activation gating in both bound and unbound channels. When the peptide binds to the ion-conducting pore, it inhibit channel opening, necessitating stronger depolarization for channel activation. We show that this activation shift could result entirely from electrostatic inhibition of the movement of the voltage-sensing S4 charges and estimate the approximate physical distance through which the S4 charges move.

Publication types

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

MeSH terms

  • Animals
  • Batrachotoxins / pharmacology
  • Calcium / pharmacology
  • Charybdotoxin / pharmacology
  • Diethylamines / pharmacology
  • Electric Conductivity
  • Electrophysiology
  • Mathematics
  • Peptides, Cyclic / metabolism
  • Peptides, Cyclic / pharmacology*
  • Rats
  • Sodium Channels / drug effects*
  • Sodium Channels / physiology*

Substances

  • Batrachotoxins
  • Diethylamines
  • Peptides, Cyclic
  • R13Q
  • Sodium Channels
  • Charybdotoxin
  • diethylamine
  • Calcium