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University of Connecticut Health Center - Know Better Care The Gregory P. Mullen NMR Structural Biology Facility & Biophysical Core Facility

ω-atracotoxin-2, a blocker of insect calcium channels

The ω-atracotoxin-2 family of toxins appear to be the most potent blockers of insect voltage-gated calcium channels reported to date. They have exceptional phylogenetic specificity, with at least a 10,000-fold preference for insect over vertebrate channels. In contrast with most other cystine knot toxins, they contain a structurally disordered, highly hydrophobic C-terminal tail which is essential for neurotoxic activity. We proposed a model in which the lipophilic tail initiates toxin binding by penetrating the membrane either adjacent to the channel or, more likely, by intercalation between transmembrane segments of the channel protein.

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Wang, X-H., Connor, M., Wilson, D., Wilson, H.I., Nicholson, G.M., Smith, R., Shaw, D., Mackay, J.P., Alewood, P.F., Christie, M.J. and King, G.F. (2001) Discovery and structure of a potent and highly specific blocker of insect calcium channels. Journal of Biological Chemistry 276, 40306-40312.

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