Scorpion toxins for the reversal of BoNT-induced paralysis.
Bioorg Med Chem Lett
; 23(24): 6743-6, 2013 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-24252544
ABSTRACT
The botulinum neurotoxins, characterized by their neuromuscular paralytic effects, are the most toxic proteins known to man. Due to their extreme potency, ease of production, and duration of activity, the BoNT proteins have been classified by the Centers for Disease Control as high threat agents for bioterrorism. In an attempt to discover effective BoNT therapeutics, we have pursued a strategy in which we leverage the blockade of K(+) channels that ultimately results in the reversal of neuromuscular paralysis. Towards this end, we utilized peptides derived from scorpion venom that are highly potent K(+) channel blockers. Herein, we report the synthesis of charybdotoxin, a 37 amino acid peptide, and detail its activity, along with iberiotoxin and margatoxin, in a mouse phrenic nerve hemidiaphragm assay in the absence and the presence of BoNT/A.
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Base de dados:
MEDLINE
Assunto principal:
Paralisia
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Nervo Frênico
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Venenos de Escorpião
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Toxinas Botulínicas
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Charibdotoxina
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Bloqueadores dos Canais de Potássio
Limite:
Animals
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article