Structurally Diverse μ-Conotoxin PIIIA Isomers Block Sodium Channel NaV1.4

Structurally Diverse μ-Conotoxin PIIIA Isomers Block Sodium Channel NaV1.4

The one and only fold? Three chemically synthesized μ‐conotoxin PIIIA isomers (see picture), which contain different disulfide connectivity, block the skeletal muscle voltage‐gated sodium channel NaV1.4 with similar, yet distinguishable potency. Hence, bioactivity of this μ‐conotoxin is not strictly...

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Veröffentlicht in:Angewandte Chemie International Edition 2012-04, Vol.51 (17), p.4058-4061
Hauptverfasser: Tietze, Alesia A., Tietze, Daniel, Ohlenschläger, Oliver, Leipold, Enrico, Ullrich, Florian, Kühl, Toni, Mischo, André, Buntkowsky, Gerd, Görlach, Matthias, Heinemann, Stefan H., Imhof, Diana
Format: Artikel
Sprache:eng
Schlagworte:
conotoxin
disulfide connectivity
NMR spectroscopy
sodium channels
structure-reactivity relationships
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Zusammenfassung:The one and only fold? Three chemically synthesized μ‐conotoxin PIIIA isomers (see picture), which contain different disulfide connectivity, block the skeletal muscle voltage‐gated sodium channel NaV1.4 with similar, yet distinguishable potency. Hence, bioactivity of this μ‐conotoxin is not strictly coupled to its native fold. Future development of conotoxin‐derived analgesics may benefit from such a widened structural repertoire.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201107011