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

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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.

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Authors and Affiliations

  1. Laboratoire de Biochimie, Ingénierie des Protéines, Faculté de Médecine Nord, CNRS UMR 6560, Boulevard Pierre Dramard, F-13916, Marseille Cédex 20, France

    Valérie Frémont, Marie-France Martin-Eauclaire & Jurphaas van Rietschoten

  2. CNRS UPR 9039, AFMB, 31 Chemin Joseph Aiguier, F-13402, Marseille Cédex 20, France

    Eric Blanc & Hervé Darbon

  3. Laboratoire de Neurobiologie, CNRS UPR 9024, 31 Chemin Joseph Aiguier, F-13402, Marseille Cédex 20, France

    Marcel Crest & Maurice Gola

Authors
  1. Valérie Frémont
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  2. Eric Blanc
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  3. Marcel Crest
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  4. Marie-France Martin-Eauclaire
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  5. Maurice Gola
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  6. Hervé Darbon
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  7. Jurphaas van Rietschoten
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Frémont, V., Blanc, E., Crest, M. et al. Dipole moments of scorpion toxins direct the interaction towards small- or large-conductance Ca2+-activated K+ channels. Lett Pept Sci 4, 305–312 (1997). https://doi.org/10.1007/BF02442894

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  • DOI: https://doi.org/10.1007/BF02442894

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