Venom-derived peptide inhibitors of voltage-gated potassium channels

Neuropharmacology. 2017 Dec:127:124-138. doi: 10.1016/j.neuropharm.2017.07.002. Epub 2017 Jul 5.

Abstract

Voltage-gated potassium channels play a key role in human physiology and pathology. Reflecting their importance, numerous channelopathies have been characterised that arise from mutations in these channels or from autoimmune attack on the channels. Voltage-gated potassium channels are also the target of a broad range of peptide toxins from venomous organisms, including sea anemones, scorpions, spiders, snakes and cone snails; many of these peptides bind to the channels with high potency and selectivity. In this review we describe the various classes of peptide toxins that block these channels and illustrate the broad range of three-dimensional structures that support channel blockade. The therapeutic opportunities afforded by these peptides are also highlighted. This article is part of the Special Issue entitled 'Venom-derived Peptides as Pharmacological Tools.'

Keywords: Cone snail; Peptide; Potassium channel; Scorpion; Sea anemone; Snake; Spider; Therapeutic.

Publication types

  • Review

MeSH terms

  • Animals
  • Peptides / chemistry
  • Peptides / pharmacology*
  • Potassium Channel Blockers / chemistry
  • Potassium Channel Blockers / pharmacology*
  • Potassium Channels, Voltage-Gated / drug effects*
  • Potassium Channels, Voltage-Gated / physiology
  • Venoms / chemistry*

Substances

  • Peptides
  • Potassium Channel Blockers
  • Potassium Channels, Voltage-Gated
  • Venoms