ArticleScientific reports2016
An insecticide resistance-breaking mosquitocide targeting inward rectifier potassium channels in vectors of Zika virus and malaria.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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Who cites it
31 citing papers in PubMed, 79 citations in OpenAlex.
- Inward Rectifier Potassium (Kir) Channel Inhibitors Protect Citrus from the Asian Citrus Psyllid by Inducing Toxicity and Inhibition of Feeding.Journal of agricultural and food chemistry · 2026Article
- Impact of Pyrethroid Resistance on the Intrinsic Insecticidal Activities of Geraniol Against the Yellow Fever Mosquito,Insects · 2026Article
- Inwardly rectifying potassium channels: Critical insights for insect species and Apis mellifera.Channels (Austin, Tex.) · 2025Review
- Contribution of glial inwardly rectifying potassium (Kir) channels to potassium buffering in insect neural systems.iScience · 2025Article
- Involvement of Inwardly Rectifying Potassium (Kir) Channels in the Toxicity of Flonicamid toInsects · 2025Article
- Identification and biophysical characterization of potential phytochemical inhibitors of carboxyl/choline esterase from Helicoverpa armigera for advancing integrated pest management strategies.Scientific reports · 2024Article
- Cloning, functional expression, and pharmacological characterization of inwardly rectifying potassium channels (Kir) from Apis mellifera.Scientific reports · 2024Article
- Potassium ion channels as a molecular target to reduce virus infection and mortality of honey bee colonies.Virology journal · 2023Article
- TargetingViruses · 2023Review
- ATP-sensitive inward rectifier potassium channels reveal functional linkage between salivary gland function and blood feeding in the mosquito, Aedes aegypti.Communications biology · 2022Article
- Aedes aegypti dyspepsia encodes a novel member of the SLC16 family of transporters and is critical for reproductive fitness.PLoS neglected tropical diseases · 2021Article
- 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
- Pesticide-Virus Interactions in Honey Bees: Challenges and Opportunities for Understanding Drivers of Bee Declines.Viruses · 2020Review
- Semi-synthetic cinnamodial analogues: Structural insights into the insecticidal and antifeedant activities of drimane sesquiterpenes against the mosquito Aedes aegypti.PLoS neglected tropical diseases · 2020Article
- Specialized stellate cells offer a privileged route for rapid water flux inProceedings of the National Academy of Sciences of the United States of America · 2020Article
- Article
- Overcoming insecticide resistance through computational inhibitor design.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- 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
- Inward rectifier potassium (Kir) channels mediate salivary gland function and blood feeding in the lone star tick, Amblyomma americanum.PLoS neglected tropical diseases · 2019Article
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Authors and funding
13 authors at 4 institutions in 1 country.
Funding
Abstract
Insecticide resistance is a growing threat to mosquito control programs around the world, thus creating the need to discover novel target sites and target-specific compounds for insecticide development. Emerging evidence suggests that mosquito inward rectifier potassium (Kir) channels represent viable molecular targets for developing insecticides with new mechanisms of action. Here we describe the discovery and characterization of VU041, a submicromolar-affinity inhibitor of Anopheles (An.) gambiae and Aedes (Ae.) aegypti Kir1 channels that incapacitates adult female mosquitoes from representative insecticide-susceptible and -resistant strains of An. gambiae (G3 and Akron, respectively) and Ae. aegypti (Liverpool and Puerto Rico, respectively) following topical application. VU041 is selective for mosquito Kir channels over several mammalian orthologs, with the exception of Kir2.1, and is not lethal to honey bees. Medicinal chemistry was used to develop an analog, termed VU730, which retains activity toward mosquito Kir1 but is not active against Kir2.1 or other mammalian Kir channels. Thus, VU041 and VU730 are promising chemical scaffolds for developing new classes of insecticides to combat insecticide-resistant mosquitoes and the transmission of mosquito-borne diseases, such as Zika virus, without harmful effects on humans and beneficial insects.
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Registered trials
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