Novel effects of dendrotoxin homologues on subtypes of mammalian Kv1 potassium channels expressed in Xenopus oocytes

FEBS Lett. 1996 Mar 25;383(1-2):26-30. doi: 10.1016/0014-5793(96)00211-6.

Abstract

We have examined the effects of two DTX homologues, toxin I and toxin K, on Kv1.1, Kv1.2 and Kv1.6 channels expressed in Xenopus oocytes. Toxin I blocked all three channels; in contrast, toxin K was selective for Kv1.1. Both toxins slowed channel activation and inactivation kinetics with 10 nM toxin I approximately doubling activation and inactivation time constants of Kv1.1. For the first time, we have demonstrated the selectivity of a DTX homologue for a single cloned Kv1 channel and suggest that these toxins may sterically hinder the conformational changes that occur during channel gating.

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Chromatography, High Pressure Liquid
  • Cloning, Molecular
  • Elapid Venoms / pharmacology*
  • Electrophysiology
  • Humans
  • Ion Channel Gating
  • Kv1.1 Potassium Channel
  • Kv1.2 Potassium Channel
  • Neurotoxins / pharmacology*
  • Oocytes
  • Patch-Clamp Techniques
  • Peptides / pharmacology*
  • Potassium Channel Blockers*
  • Potassium Channels / genetics
  • Potassium Channels / metabolism
  • Potassium Channels, Voltage-Gated*
  • Rats
  • Xenopus laevis

Substances

  • Elapid Venoms
  • KCNA1 protein, human
  • KCNA2 protein, human
  • Kcna2 protein, rat
  • Kv1.2 Potassium Channel
  • Neurotoxins
  • Peptides
  • Potassium Channel Blockers
  • Potassium Channels
  • Potassium Channels, Voltage-Gated
  • dendrotoxin K
  • Kv1.1 Potassium Channel
  • dendrotoxin