Compound-specific effects of mutations at Val787 in DII-S6 of Nav 1.4 sodium channels on the action of sodium channel inhibitor insecticides.

@article{Stein2012CompoundspecificEO,
  title={Compound-specific effects of mutations at Val787 in DII-S6 of Nav 1.4 sodium channels on the action of sodium channel inhibitor insecticides.},
  author={Richard T von Stein and David M. Soderlund},
  journal={Neurotoxicology},
  year={2012},
  volume={33 5},
  pages={1381-9}
}
Sodium channel inhibitor (SCI) insecticides are hypothesized to inhibit voltage-gated sodium channels by binding selectively to the slow-inactivated state. Replacement of valine at position 787 in the S6 segment of homology domain II of the rat Na(v)1.4 sodium channel by lysine (V787K) enchances slow inactivation of this channel whereas replacement by alanine or cysteine (V787A and V787C) inhibits slow inactivation. To test the hypothesis that SCI insecticides bind selectively to the slow… CONTINUE READING

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