TY - JOUR
T1 - The depressant scorpion neurotoxin LqqIT2 selectively modulates the insect voltage-gated sodium channel
AU - Bosmans, Frank
AU - Martin-Eauclaire, Marie France
AU - Tytgat, Jan
N1 - Funding Information:
We would like to thank the following persons: Martin S. Williamson, IACR-Rothamsted, UK for sharing the para and tipE clone; A.L. Goldin, University of California, Irvine, USA for sharing Na v 1.2 and S.H. Heinemann, Friedrich-Schiller-Universität Jena, Germany for sharing the β 1 subunit. We thank C. Maertens for helpful discussions. This work was supported by grant G.0081.02 (F.W.O. Vlaanderen).
PY - 2005/3/15
Y1 - 2005/3/15
N2 - LqqIT2 is a depressant neurotoxin present in the venom of the Leiurus quinquestriatus quinquestriatus scorpion, one of the world's most dangerous scorpions endemic to dry habitats in Africa and Asia. In order to determine its efficacy, potency and selectivity, LqqIT2 was subjected for the first time to an electrophysiological and pharmacological comparison between two different cloned sodium channels expressed in Xenopus laevis oocytes. Aside from typical β-toxin effects, LqqIT2 also affected the inactivation process and ion selectivity of the insect voltage-gated sodium channel. The most interesting feature of LqqIT2 is its total insect-selectivity. At a concentration of 1 μM, the insect-voltage-gated sodium channel, para, was profoundly modulated while its mammalian counterpart, the rat brain Nav1.2 channel, was not affected. This trait offers excellent prospects for the development of novel insecticides.
AB - LqqIT2 is a depressant neurotoxin present in the venom of the Leiurus quinquestriatus quinquestriatus scorpion, one of the world's most dangerous scorpions endemic to dry habitats in Africa and Asia. In order to determine its efficacy, potency and selectivity, LqqIT2 was subjected for the first time to an electrophysiological and pharmacological comparison between two different cloned sodium channels expressed in Xenopus laevis oocytes. Aside from typical β-toxin effects, LqqIT2 also affected the inactivation process and ion selectivity of the insect voltage-gated sodium channel. The most interesting feature of LqqIT2 is its total insect-selectivity. At a concentration of 1 μM, the insect-voltage-gated sodium channel, para, was profoundly modulated while its mammalian counterpart, the rat brain Nav1.2 channel, was not affected. This trait offers excellent prospects for the development of novel insecticides.
KW - Depressant scorpion toxin
KW - Insecticide
KW - LqqIT2
UR - http://www.scopus.com/inward/record.url?scp=13944258544&partnerID=8YFLogxK
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U2 - 10.1016/j.toxicon.2004.12.010
DO - 10.1016/j.toxicon.2004.12.010
M3 - Article
C2 - 15733572
AN - SCOPUS:13944258544
SN - 0041-0101
VL - 45
SP - 501
EP - 507
JO - Toxicon
JF - Toxicon
IS - 4
ER -