Structurally Diverse mu -Conotoxin PIIIA Isomers Block Sodium Channel Na sub(V)1.4

Structurally Diverse mu -Conotoxin PIIIA Isomers Block Sodium Channel Na sub(V)1.4

The one and only fold? Three chemically synthesized mu -conotoxin PIIIA isomers (see picture), which contain different disulfide connectivity, block the skeletal muscle voltage-gated sodium channel Na sub(V)1.4 with similar, yet distinguishable potency. Hence, bioactivity of this mu -conotoxin is no...

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Veröffentlicht in:Angewandte Chemie International Edition 2012-04, Vol.51 (17), p.4058-4061
Hauptverfasser: Tietze, Alesia A, Tietze, Daniel, Ohlenschlaeger, Oliver, Leipold, Enrico, Ullrich, Florian, Kuehl, Toni, Mischo, Andre, Buntkowsky, Gerd, Gorlach, Matthias, Heinemann, Stefan H, Imhof, Diana
Format: Artikel
Sprache:eng
Schlagworte:
Biochemistry
Blocking
Channels
Disulfides
Isomers
Joining
Muscles
Sodium
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Beschreibung
Zusammenfassung:The one and only fold? Three chemically synthesized mu -conotoxin PIIIA isomers (see picture), which contain different disulfide connectivity, block the skeletal muscle voltage-gated sodium channel Na sub(V)1.4 with similar, yet distinguishable potency. Hence, bioactivity of this mu -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