ArticlePloS one2014
Pharmacological validation of an inward-rectifier potassium (Kir) channel as an insecticide target in the yellow fever mosquito Aedes aegypti.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 44 citations in OpenAlex.
- Inwardly rectifying potassium channels: Critical insights for insect species and Apis mellifera.Channels (Austin, Tex.) · 2025Review
- Physiological and Putative Organic Cation Transporter Expression Response to Alizarin Dye Exposure inInsects · 2025Article
- The Elongation Factor 1 Alpha Promoter Drives the Functional Expression of Kir2A inInternational journal of molecular sciences · 2025Article
- Involvement of Inwardly Rectifying Potassium (Kir) Channels in the Toxicity of Flonicamid toInsects · 2025Article
- Further SAR on the (Phenylsulfonyl)piperazine Scaffold as Inhibitors of the Aedes aegypti Kir1 (AeKir) Channel and Larvicides.ChemMedChem · 2021Article
- Phylogenomics of Tick Inward Rectifier Potassium Channels and Their Potential as Targets to Innovate Control Technologies.Frontiers in cellular and infection microbiology · 2021Review
- Article
- Discovery and Characterization of 2-Nitro-5-(4-(phenylsulfonyl)piperazin-1-yl)- N-(pyridin-4-ylmethyl)anilines as Novel Inhibitors of the Aedes aegypti Kir1 ( AeKir1) Channel.ACS infectious diseases · 2019Article
- Pharmacological Inhibition of Inward Rectifier Potassium Channels Induces Lethality in LarvalInsects · 2018Article
- Inward rectifier potassium (Kir) channels in the soybean aphid Aphis glycines: Functional characterization, pharmacology, and toxicology.Journal of insect physiology · 2018Article
- Development of an autodissemination strategy for the deployment of novel control agents targeting the common malaria mosquito, Anopheles quadrimaculatus say (Diptera: Culicidae).PLoS neglected tropical diseases · 2018Article
- Analysis of the Aedes albopictus C6/36 genome provides insight into cell line utility for viral propagation.GigaScience · 2018Article
- A natural agonist of mosquito TRPA1 from the medicinal plant Cinnamosma fragrans that is toxic, antifeedant, and repellent to the yellow fever mosquito Aedes aegypti.PLoS neglected tropical diseases · 2018Article
- Inwardly Rectifying Potassium (Kir) Channels Represent a Critical Ion Conductance Pathway in the Nervous Systems of Insects.Scientific reports · 2018Article
- ATP-sensitive inwardly rectifying potassium channel regulation of viral infections in honey bees.Scientific reports · 2017Article
- Malpighian Tubules as Novel Targets for Mosquito Control.International journal of environmental research and public health · 2017Review
- An insecticide resistance-breaking mosquitocide targeting inward rectifier potassium channels in vectors of Zika virus and malaria.Scientific reports · 2016Article
- Two inwardly rectifying potassium channels, Irk1 and Irk2, play redundant roles in Drosophila renal tubule function.American journal of physiology. Regulatory, integrative and comparative physiology · 2015Article
- Excretion of NaCl and KCl loads in mosquitoes. 2. Effects of the small molecule Kir channel modulator VU573 and its inactive analog VU342.American journal of physiology. Regulatory, integrative and comparative physiology · 2014Article
- Discovery and characterization of a potent and selective inhibitor of Aedes aegypti inward rectifier potassium channels.PloS one · 2014Article
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
Abstract
Mosquitoes are important disease vectors that transmit a wide variety of pathogens to humans, including those that cause malaria and dengue fever. Insecticides have traditionally been deployed to control populations of disease-causing mosquitoes, but the emergence of insecticide resistance has severely limited the number of active compounds that are used against mosquitoes. Thus, to improve the control of resistant mosquitoes there is a need to identify new insecticide targets and active compounds for insecticide development. Recently we demonstrated that inward rectifier potassium (Kir) channels and small molecule inhibitors of Kir channels offer promising new molecular targets and active compounds, respectively, for insecticide development. Here we provide pharmacological validation of a specific mosquito Kir channel (AeKir1) in the yellow fever mosquito Aedes aegypti. We show that VU590, a small-molecule inhibitor of mammalian Kir1.1 and Kir7.1 channels, potently inhibits AeKir1 but not another mosquito Kir channel (AeKir2B) in vitro. Moreover, we show that a previously identified inhibitor of AeKir1 (VU573) elicits an unexpected agonistic effect on AeKir2B in vitro. Injection of VU590 into the hemolymph of adult female mosquitoes significantly inhibits their capacity to excrete urine and kills them within 24 h, suggesting a mechanism of action on the excretory system. Importantly, a structurally-related VU590 analog (VU608), which weakly blocks AeKir1 in vitro, has no significant effects on their excretory capacity and does not kill mosquitoes. These observations suggest that the toxic effects of VU590 are associated with its inhibition of AeKir1.
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