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Letters in Peptide Science

, Volume 4, Issue 4–6, pp 305–312 | Cite as

Dipole moments of scorpion toxins direct the interaction towards small- or large-conductance Ca2+-activated K+ channels

  • Valérie Frémont
  • Eric Blanc
  • Marcel Crest
  • Marie-France Martin-Eauclaire
  • Maurice Gola
  • Hervé Darbon
  • Jurphaas van Rietschoten
Article

Summary

Ca2+-activated K+ channels consist of a large family of membrane proteins, among which two groups have been characterized by electrophysiological criteria, the small conductance (SK) and the large conductance (BK) Ca2+-activated K+ channels. Scorpion toxins that block K+ channels exhibit a common three-dimensional structure constituted of a short α-helix connected by disulfide bonds to a β-sheet. The leiurotoxin I (LTX1) related toxins interact specifically with the SK channel via basic residues of their α-helix, while the charybdotoxin (ChTX) family recognizes the BK channel with basic residues of their β-sheet. In an attempt to better understand the structure-activity relationships of these toxins and the characteristics of the electrostatic interactions with the receptor site, we investigated the electrostatic potential supported by natural toxins and a synthetic analogue to find out if it may help in understanding the molecular mechanisms involved in this peptide-protein interaction.

Keywords

Electrostatic interactions Iberiotoxin K+ channel blockers Leiurotoxin Peptide-receptor interaction Scorpion toxins 

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Copyright information

© Kluwer Academic Publishers 1997

Authors and Affiliations

  • Valérie Frémont
    • 1
  • Eric Blanc
    • 2
  • Marcel Crest
    • 3
  • Marie-France Martin-Eauclaire
    • 1
  • Maurice Gola
    • 3
  • Hervé Darbon
    • 2
  • Jurphaas van Rietschoten
    • 1
  1. 1.Laboratoire de Biochimie, Ingénierie des Protéines, Faculté de Médecine NordCNRS UMR 6560Marseille Cédex 20France
  2. 2.CNRS UPR 9039AFMBMarseille Cédex 20France
  3. 3.Laboratoire de NeurobiologieCNRS UPR 9024Marseille Cédex 20France

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