"The King is dead": Checkmating ion channels with tethered toxins

Toxicon. 2010 Dec;56(8):1293-8. doi: 10.1016/j.toxicon.2010.09.016. Epub 2010 Oct 7.


The quickest possible checkmate in the game of chess requires two moves using a pawn and the queen. Metaphorically speaking, the pawn (a membrane tether) and the queen (a toxin) work together to checkmate an ion channel within a neuronal circuit. This strategy termed "tethered toxin" (t-toxin) is based on the use of genetically encoded peptide toxins that are anchored to the cell-membrane via a glycolipid or transmembrane tether. Because of their mode of action at the cell surface, t-toxins act only on ion channels and receptors of the cell that is expressing the t-toxin, and not on identical receptors present in neighboring cells that do not express the t-toxin. In this mini-review we discuss the design of these genetic tools and their application for cell-specific and temporal manipulation of ion channel-mediated activities in vivo.

Publication types

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

MeSH terms

  • Animals
  • Cell Membrane / metabolism
  • Humans
  • Ion Channel Gating / genetics
  • Ion Channel Gating / physiology
  • Ion Channels / antagonists & inhibitors*
  • Ion Transport / genetics
  • Ion Transport / physiology
  • Membrane Transport Modulators / chemistry*
  • Membrane Transport Modulators / metabolism
  • Mice
  • Models, Biological
  • Models, Molecular
  • Neurotransmitter Agents / metabolism
  • Organisms, Genetically Modified / metabolism
  • Rats
  • Substrate Specificity
  • Toxins, Biological / chemistry*
  • Toxins, Biological / genetics
  • Toxins, Biological / physiology
  • Venoms / chemistry*
  • Venoms / genetics
  • Zebrafish / metabolism


  • Ion Channels
  • Membrane Transport Modulators
  • Neurotransmitter Agents
  • Toxins, Biological
  • Venoms