ArticleThe Journal of biological chemistry2016
The Receptor Site and Mechanism of Action of Sodium Channel Blocker Insecticides.
Article in The Journal of biological chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
12 citing papers in PubMed, 34 citations in OpenAlex.
- Whole-Genome Resequencing of the VGSC Reveals the Evolutionary Mechanism of Pesticide Resistance inInternational journal of molecular sciences · 2026Article
- Toward Overcoming Pyrethroid Resistance in Mosquito Control: The Role of Sodium Channel Blocker Insecticides.International journal of molecular sciences · 2023Article
- Susceptibility Evaluation of Fall Armyworm (Journal of toxicology · 2022Article
- Naview: A d3.js Based JavaScript Library for Drawing and Annotating Voltage-Gated Sodium Channels Membrane Diagrams.Frontiers in bioinformatics · 2022Article
- Spatial Anopheles arabiensis (Diptera: Culicidae) insecticide resistance patterns across malaria-endemic regions of Botswana.Malaria journal · 2020Article
- Establishment of cumulative assessment groups of pesticides for their effects on the nervous system.EFSA journal. European Food Safety Authority · 2019Article
- Optical control of L-type CaNature chemical biology · 2018Article
- Treatment with pentylenetetrazole (PTZ) and 4-aminopyridine (4-AP) differently affects survival, locomotor activity, and biochemical markers in Drosophila melanogaster.Molecular and cellular biochemistry · 2018Article
- Synthesis and Acaricidal Activities of Scopoletin Phenolic Ether Derivatives: QSAR, Molecular Docking Study and in Silico ADME Predictions.Molecules (Basel, Switzerland) · 2018Article
- Insecticide Resistance Associated withBioMed research international · 2018Review
- Insect-Active Toxins with Promiscuous Pharmacology from the African Theraphosid Spider Monocentropus balfouri.Toxins · 2017Article
- Molecular Mechanism of Action and Selectivity of Sodium Ch annel Blocker Insecticides.Current medicinal chemistry · 2017Review
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 4 countries.
Funding
Abstract
Sodium channels are excellent targets of both natural and synthetic insecticides with high insect selectivity. Indoxacarb, its active metabolite DCJW, and metaflumizone (MFZ) belong to a relatively new class of sodium channel blocker insecticides (SCBIs) with a mode of action distinct from all other sodium channel-targeting insecticides, including pyrethroids. Electroneutral SCBIs preferably bind to and trap sodium channels in the inactivated state, a mechanism similar to that of cationic local anesthetics. Previous studies identified several SCBI-sensing residues that face the inner pore of sodium channels. However, the receptor site of SCBIs, their atomic mechanisms, and the cause of selective toxicity of MFZ remain elusive. Here, we have built a homology model of the open-state cockroach sodium channel BgNav1-1a. Our computations predicted that SCBIs bind in the inner pore, interact with a sodium ion at the focus of P1 helices, and extend their aromatic moiety into the III/IV domain interface (fenestration). Using model-driven mutagenesis and electrophysiology, we identified five new SCBI-sensing residues, including insect-specific residues. Our study proposes the first three-dimensional models of channel-bound SCBIs, sheds light on the molecular basis of MFZ selective toxicity, and suggests that a sodium ion located in the inner pore contributes to the receptor site for electroneutral SCBIs.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.