Two novel ergtoxins, blockers of K+-channels, purified from the Mexican scorpion Centruroides elegans elegans

Neurochem Res. 2008 Aug;33(8):1525-33. doi: 10.1007/s11064-008-9634-8. Epub 2008 Mar 13.

Abstract

Voltage-gated potassium channels of the ether-a-go-go related gene (ERG) family are implicated in many important cellular processes. Three such genes have been cloned (erg1, erg2 and erg3) and shown to be expressed in the central nervous system (CNS) of mammalians. This communication describes the isolation and characterization of two isoforms of scorpion toxin (CeErg4 and CeErg5, systematic nomenclature gamma-KTx1.7 and gamma-KTx1.8, respectively) that can discriminate the various subtypes of ERG channels of human and rat. These peptides were purified from the venom of the Mexican scorpion Centruroides elegans elegans. They contain 42 amino acid residues, tightly folded by four disulfide bridges. Both peptides block in a reversible manner human and rat ERG1 channels, but have no effect on human ERG2. They also block completely and irreversibly the rat ERG2 and the human ERG3 channels hence are excellent tools for the discrimination of the various sub-types of ion-channels studied.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Ether-A-Go-Go Potassium Channels / genetics
  • Ether-A-Go-Go Potassium Channels / metabolism*
  • Humans
  • Molecular Sequence Data
  • Patch-Clamp Techniques
  • Peptides / genetics
  • Peptides / isolation & purification*
  • Peptides / metabolism*
  • Potassium Channel Blockers* / isolation & purification
  • Potassium Channel Blockers* / metabolism
  • Rats
  • Scorpion Venoms / genetics
  • Scorpion Venoms / isolation & purification*
  • Scorpion Venoms / metabolism*
  • Scorpions / chemistry*
  • Sequence Alignment

Substances

  • Centruroides toxin
  • Ether-A-Go-Go Potassium Channels
  • Peptides
  • Potassium Channel Blockers
  • Scorpion Venoms
  • ergtoxin 4, Centruroides elegans
  • ergtoxin 5, Centruroides elegans