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A toxin to nervous, cardiac, and endocrine ERG K + channels isolated from Centruroides noxius scorpion venom

1999; Wiley; Volume: 13; Issue: 8 Linguagem: Inglês

10.1096/fasebj.13.8.953

1530-6860

Georgina B. Gurrola, Barbara Rosati, Marcella Rocchetti, Genaro Pimienta, Antonio Zaza, Annarosa Arcangeli, Massimo Olivotto, Lourival D. Possani, Enzo Wanke,

Nicotinic Acetylcholine Receptors Study

Toxins isolated from a variety of venoms are tools for probing the physiological function and structure of ion channels. The ether-a-go-go-related genes (erg) codify for the K+ channels (ERG), which are crucial in neurons and are impaired in human long-QT syndrome and Drosophila 'seizure' mutants. We have isolated a peptide from the scorpion Centruroides noxius Hoffmann that has no sequence homologies with other toxins, and demonstrate that it specifically inhibits (IC50 = 16±1 nM) only ERG channels of different species and distinct histogenesis. These results open up the possibility of investigating ERG channel structure-function relationships and novel pharmacological tools with potential therapeutic efficacy.—Gurrola, G. B., Rosati, B., Rocchetti, M., Pimienta, G., Zaza, A., Arcangeli, A., Olivotto, M., Possani, L. D., Wanke, E. A toxin to nervous, cardiac, and endocrine ERG K+ channels isolated from Centruroides noxius scorpion venom. FASEB J. 13, 953–962 (1999)