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Three-dimensional structure of scorpion toxins: Towards a new model of interaction with potassium channels

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Perspectives in Drug Discovery and Design

Abstract

Scorpion venom contains various toxins which block ion-channels, responsible for either sodium, potassium, calcium or chloride membrane permeation. This review focuses on the three-dimensional structure of scorpion toxins specific for potassium channels, and on their structure–activity relationships. The overall fold of all these toxins is similar, despite their various specificities towards different types of potassium channels. Fine studies of the influence of punctual mutations of both toxins and channels have converged on a precise description of the scorpion toxins functional maps. From this knowledge, it now becomes possible to predict the specificity of a newly described scorpion toxin. The way is thus now open that leads to the design of new potent synthetic potassium channel blockers which in turn could be used as therapeutic drugs.

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Authors and Affiliations

  1. AFMB, CNRS UPR 9039, IFR1, 31, Chemin Joseph-Aiguier, F-13402, Marseille Cedex 20, France

    H. Darbon & E. Blanc

  2. Faculté de Médecine-Nord, CNRS UMR 6560-IFR Jean-Roche, Bd. Pierre Dramard, F-13916, Marseille Cedex 20, France

    J.-M. Sabatier

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  1. H. Darbon
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Darbon, H., Blanc, E. & Sabatier, JM. Three-dimensional structure of scorpion toxins: Towards a new model of interaction with potassium channels. Perspectives in Drug Discovery and Design 15, 41–60 (1999). https://doi.org/10.1023/A:1017070801207

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