Journal ArticleInsect science · December 2023
Drosophila sodium channel 1 (DSC1) encodes a voltage-gated divalent cation channel that mediates neuronal excitability in insects. Previous research revealed that DSC1 knockout Drosophila melanogaster conferred different susceptibility to insecticides, whi ...
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Journal ArticleNature · September 2023
Many animal- and plant-pathogenic bacteria use a type III secretion system to deliver effector proteins into host cells1,2. Elucidation of how these effector proteins function in host cells is critical for understanding infectious diseases in animals and p ...
Full textOpen AccessLink to itemCite
Journal ArticleACS infectious diseases · July 2023
The development of safe and potent insecticides remains an integral part of a multifaceted strategy to effectively control human-disease-transmitting insect vectors. Incorporating fluorine can dramatically alter the physiochemical properties and bioavailab ...
Full textCite
Journal ArticlePesticide biochemistry and physiology · May 2023
Mosquito-borne diseases are an increasing global health challenge and vector-based interventions remain the most important methods for reducing the public health burden of most mosquito-borne diseases. Transfluthrin, a volatile pyrethroid insecticide, is u ...
Full textCite
Journal ArticleInsect biochemistry and molecular biology · September 2022
Pyrethroid insecticides prolong the opening of insect sodium channels by binding to two predicted pyrethroid receptor sites (PyR), PyR1 and PyR2. Many naturally-occurring sodium channel mutations that confer pyrethroid resistance (known as knockdown resist ...
Full textCite
Journal ArticleInsects · August 2022
Pyrethroid insecticides stabilize the open state of insect sodium channels. Previous mutational, electrophysiological, and computational analyses led to the development of homology models predicting two pyrethroid receptor sites, PyR1 and PyR2. Many of the ...
Full textCite
Journal ArticleInsect science · June 2022
Voltage-gated sodium channels are the primary target of pyrethroid insecticides. Mutations in sodium channel confer knockdown resistance (kdr) to pyrethroids in various arthropod pests. Haedoxan A (HA) is the major insecticidal component from Phryma leptos ...
Full textCite
Journal ArticlePest management science · February 2022
BackgroundUse of pyrethroid insecticides is a pivotal strategy for mosquito control globally. Commonly known for their insecticidal activity by acting on voltage-gated sodium channels, pyrethroids, such as bioallethrin and transfluthrin, are used ...
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Journal ArticleInsect science · December 2021
The phenylpyrazole insecticide fipronil blocks resistance to dieldrin (RDL) γ-aminobutyric acid (GABA) receptors in insects, thereby impairing inhibitory neurotransmission. Some insect species, such as the diamondback moth (Plutella xylostella), possess mo ...
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Journal ArticleInsect biochemistry and molecular biology · October 2021
Scorpion α-toxins bind at the pharmacologically-defined site-3 on the sodium channel and inhibit channel inactivation by preventing the outward movement of the voltage sensor in domain IV (IVS4), whereas scorpion β-toxins bind at site-4 on the sodium chann ...
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Journal ArticlePest management science · August 2021
Featured Publication
BackgroundInsects rely on their sense of smell to locate food and hosts, find mates and select sites for laying eggs. Use of volatile compounds, such as essential oils (EOs), to repel insect pests and disrupt their olfaction-driven behaviors has g ...
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Journal ArticlePest management science · August 2021
BackgroundPyrethrum from dry flowers of Chrysanthemum is a well-known botanical insecticide and repellent. Its insecticidal activity attributes to its six insecticidal esters, collectively known as pyrethrins. Pyrethrins and its synthetic analogs ...
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Journal ArticlePLoS neglected tropical diseases · July 2021
BackgroundVolatile pyrethroid insecticides, such as transfluthrin, have received increasing attention for their potent repellent activities in recent years for controlling human disease vectors. It has been long understood that pyrethroids kill in ...
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Journal ArticlePLoS genetics · July 2021
Pyrethrum extract from dry flowers of Tanacetum cinerariifolium (formally Chrysanthemum cinerariifolium) has been used globally as a popular insect repellent against arthropod pests for thousands of years. However, the mechanistic basis of pyrethrum repell ...
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Journal ArticleThe Biochemical journal · July 2021
The interaction of insect-selective scorpion depressant β-toxins (LqhIT2 and Lqh-dprIT3 from Leiurus quinquestriatus hebraeus) with the Blattella germanica sodium channel, BgNav1-1a, was investigated using site-directed mutagenesis, electrophysiological an ...
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Journal ArticleNature communications · May 2021
Pyrethrum extracts from flower heads of Chrysanthemum spp. have been used worldwide in insecticides and repellents. While the molecular mechanisms of its insecticidal action are known, the molecular basis of pyrethrum repellency remains a mystery. In this ...
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Journal ArticleInsect biochemistry and molecular biology · August 2020
Voltage-gated sodium channels are the major targets of several classes of insecticides, including pyrethroids. However, sensitivities of many insect pest species to pyrethroids have gradually decreased due to overuse in pest management programs. One major ...
Full textCite
Journal ArticleArchives of insect biochemistry and physiology · June 2020
Aedes aegypti is the primary mosquito vector of dengue, yellow fever, Zika and chikungunya. Current strategies to control Ae. aegypti rely heavily on insecticide interventions. Pyrethroids are a major class of insecticides used for mosquito control because ...
Full textCite
Journal ArticleInsect science · December 2023
Drosophila sodium channel 1 (DSC1) encodes a voltage-gated divalent cation channel that mediates neuronal excitability in insects. Previous research revealed that DSC1 knockout Drosophila melanogaster conferred different susceptibility to insecticides, whi ...
Full textCite
Journal ArticleNature · September 2023
Many animal- and plant-pathogenic bacteria use a type III secretion system to deliver effector proteins into host cells1,2. Elucidation of how these effector proteins function in host cells is critical for understanding infectious diseases in animals and p ...
Full textOpen AccessLink to itemCite
Journal ArticleACS infectious diseases · July 2023
The development of safe and potent insecticides remains an integral part of a multifaceted strategy to effectively control human-disease-transmitting insect vectors. Incorporating fluorine can dramatically alter the physiochemical properties and bioavailab ...
Full textCite
Journal ArticlePesticide biochemistry and physiology · May 2023
Mosquito-borne diseases are an increasing global health challenge and vector-based interventions remain the most important methods for reducing the public health burden of most mosquito-borne diseases. Transfluthrin, a volatile pyrethroid insecticide, is u ...
Full textCite
Journal ArticleInsect biochemistry and molecular biology · September 2022
Pyrethroid insecticides prolong the opening of insect sodium channels by binding to two predicted pyrethroid receptor sites (PyR), PyR1 and PyR2. Many naturally-occurring sodium channel mutations that confer pyrethroid resistance (known as knockdown resist ...
Full textCite
Journal ArticleInsects · August 2022
Pyrethroid insecticides stabilize the open state of insect sodium channels. Previous mutational, electrophysiological, and computational analyses led to the development of homology models predicting two pyrethroid receptor sites, PyR1 and PyR2. Many of the ...
Full textCite
Journal ArticleInsect science · June 2022
Voltage-gated sodium channels are the primary target of pyrethroid insecticides. Mutations in sodium channel confer knockdown resistance (kdr) to pyrethroids in various arthropod pests. Haedoxan A (HA) is the major insecticidal component from Phryma leptos ...
Full textCite
Journal ArticlePest management science · February 2022
BackgroundUse of pyrethroid insecticides is a pivotal strategy for mosquito control globally. Commonly known for their insecticidal activity by acting on voltage-gated sodium channels, pyrethroids, such as bioallethrin and transfluthrin, are used ...
Full textCite
Journal ArticleInsect science · December 2021
The phenylpyrazole insecticide fipronil blocks resistance to dieldrin (RDL) γ-aminobutyric acid (GABA) receptors in insects, thereby impairing inhibitory neurotransmission. Some insect species, such as the diamondback moth (Plutella xylostella), possess mo ...
Full textCite
Journal ArticleInsect biochemistry and molecular biology · October 2021
Scorpion α-toxins bind at the pharmacologically-defined site-3 on the sodium channel and inhibit channel inactivation by preventing the outward movement of the voltage sensor in domain IV (IVS4), whereas scorpion β-toxins bind at site-4 on the sodium chann ...
Full textCite
Journal ArticlePest management science · August 2021
Featured Publication
BackgroundInsects rely on their sense of smell to locate food and hosts, find mates and select sites for laying eggs. Use of volatile compounds, such as essential oils (EOs), to repel insect pests and disrupt their olfaction-driven behaviors has g ...
Full textCite
Journal ArticlePest management science · August 2021
BackgroundPyrethrum from dry flowers of Chrysanthemum is a well-known botanical insecticide and repellent. Its insecticidal activity attributes to its six insecticidal esters, collectively known as pyrethrins. Pyrethrins and its synthetic analogs ...
Full textCite
Journal ArticlePLoS neglected tropical diseases · July 2021
BackgroundVolatile pyrethroid insecticides, such as transfluthrin, have received increasing attention for their potent repellent activities in recent years for controlling human disease vectors. It has been long understood that pyrethroids kill in ...
Full textCite
Journal ArticlePLoS genetics · July 2021
Pyrethrum extract from dry flowers of Tanacetum cinerariifolium (formally Chrysanthemum cinerariifolium) has been used globally as a popular insect repellent against arthropod pests for thousands of years. However, the mechanistic basis of pyrethrum repell ...
Full textCite
Journal ArticleThe Biochemical journal · July 2021
The interaction of insect-selective scorpion depressant β-toxins (LqhIT2 and Lqh-dprIT3 from Leiurus quinquestriatus hebraeus) with the Blattella germanica sodium channel, BgNav1-1a, was investigated using site-directed mutagenesis, electrophysiological an ...
Full textCite
Journal ArticleNature communications · May 2021
Pyrethrum extracts from flower heads of Chrysanthemum spp. have been used worldwide in insecticides and repellents. While the molecular mechanisms of its insecticidal action are known, the molecular basis of pyrethrum repellency remains a mystery. In this ...
Full textCite
Journal ArticleInsect biochemistry and molecular biology · August 2020
Voltage-gated sodium channels are the major targets of several classes of insecticides, including pyrethroids. However, sensitivities of many insect pest species to pyrethroids have gradually decreased due to overuse in pest management programs. One major ...
Full textCite
Journal ArticleArchives of insect biochemistry and physiology · June 2020
Aedes aegypti is the primary mosquito vector of dengue, yellow fever, Zika and chikungunya. Current strategies to control Ae. aegypti rely heavily on insecticide interventions. Pyrethroids are a major class of insecticides used for mosquito control because ...
Full textCite
Journal ArticleInsect biochemistry and molecular biology · March 2020
Voltage-gated sodium channels (Nav) are essential for electrical signaling in the nervous system. They are also the primary targets of several classes of insecticides including pyrethroids. There is only one sodium channel gene in most insect sp ...
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Journal ArticleJournal of agricultural and food chemistry · July 2019
Indoxacarb, a commercialized oxadiazine insecticide, nearly irreversibly blocks open/inactivated, but not resting sodium channels. The structure-activity relationships showed that the substituents at the position of the chiral atom in the oxadiazine ring a ...
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Journal ArticlePLoS neglected tropical diseases · June 2019
BackgroundMultiple mutations in the voltage-gated sodium channel have been associated with knockdown resistance (kdr) to DDT and pyrethroid insecticides in a major human disease vector Aedes aegypti. One mutation, V1016G, confers sodium channel re ...
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Journal ArticlePesticide biochemistry and physiology · October 2018
Pyrethrin I, pyrethrin II, cinerin I, cinerin II, jasmolin I and jasmolin II are six closely related insecticidal active esters, known as pyrethrins, found in the pyrethrum extract from the dry flowers of Tanacetum cinerariifolium. The chemical structures ...
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Journal ArticleArchives of biochemistry and biophysics · August 2018
Voltage-gated sodium channels have residues that change or may change contacts upon gating. Contributions of individual contacts in stability of different states are incompletely understood. Pore-lining inner helices contain exceptionally conserved asparag ...
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Journal ArticleInsect biochemistry and molecular biology · August 2018
Flonicamid is a selective insecticide for the control of sap-sucking insects; it exerts toxic effects by inhibiting insect feeding. However, its molecular target remains elusive. In this study, we functionally characterized NlKir1 channels of the brown pla ...
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Journal ArticlePesticide biochemistry and physiology · June 2018
Pyrethroid insecticides modify the gating of voltage-gated sodium channels, thus disrupting the function of the nervous system. In Drosophila melanogaster, para encodes a functional sodium channel. Drosophila Sodium Channel 1 (DSC1), although considered as ...
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Journal ArticleEnvironmental entomology · June 2018
Drosophila suzukii (Matsumura) (Diptera: Drosophilidae) is a devastating global pest of berry crops and cherries. Little is understood about its biology during the winter in northern temperate regions, including potential resources that it may utilize duri ...
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Journal ArticleBulletin of Insectology · January 1, 2018
The study was conducted to evaluate whether Bemisia tabaci (Gennadius) (MEAM1, formerly B biotype) populations in Turkey have developed resistance to neonicotinoid insecticides. We collected B. tabaci from vegetable and cotton growing areas in the Mediterr ...
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Journal ArticleProceedings of the National Academy of Sciences of the United States of America · December 2017
Insecticides are widely used to control pests in agriculture and insect vectors that transmit human diseases. However, these chemicals can have a negative effect on nontarget, beneficial organisms including bees. Discovery and deployment of selective insec ...
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Journal ArticleActa Horticulturae · July 25, 2017
Pyrethroid insecticides have been used extensively in controlling arthropod pests and disease vectors. They act on voltage-gated sodium channels, which are essential for the initiation and propagation of the action potential in neurons and other excitable ...
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Journal ArticleNeurotoxicology · May 2017
Pyrethroid insecticides exert toxic effects by prolonging the opening of voltage-gated sodium channels. More than 20 sodium channel mutations from arthropod pests and disease vectors have been confirmed to confer pyrethroid resistance. These mutations have ...
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Journal ArticleNeurotoxicology · May 2017
DDT and pyrethroid insecticides were among the earliest neurotoxins identified to act on voltage-gated sodium channels. In the 1960s, equipped with, at the time, new voltage-clamp techniques, Professor Narahashi and associates provided the initial evidence ...
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Journal ArticleScientific reports · April 2017
The yellow fever mosquito, Aedes aegypti, particularly in Neotropical regions, is the principal vector of dengue, yellow fever, Zika and Chikungunya viruses. Pyrethroids remain one of the most used insecticides to control Aedes mosquitoes, despite the deve ...
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Journal ArticleInsect biochemistry and molecular biology · March 2017
Mutations in sodium channels are known to confer knockdown resistance to pyrethroid insecticides, such as permethrin and cypermethrin, in various agricultural pests and disease vectors. Double mutations, D3i28V and E3i32G, were detect ...
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Journal ArticleCurrent medicinal chemistry · January 2017
Sodium channel blocker insecticides (SCBIs) are a relatively new class of insecticides that are represented by two commercially registered compounds, indoxacarb and metaflumizone. SCBIs, like pyrethroids and DDT, target voltage-gated sodium channels (VGSCs ...
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Journal ArticleInsects · October 2016
Pyrethroid insecticides are widely used to control insect pests and human disease vectors. Voltage-gated sodium channels are the primary targets of pyrethroid insecticides. Mutations in the sodium channel have been shown to be responsible for pyrethroid re ...
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Journal ArticleThe Journal of biological chemistry · September 2016
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) w ...
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Journal ArticleToxins · February 2016
Haedoxan A (HA) is a major active ingredient in the herbaceous perennial plant lopseed (Phryma leptostachya L.), which is used as a natural insecticide against insect pests in East Asia. Here, we report that HA delayed the decay rate of evoked excitatory j ...
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Journal ArticleThe Journal of biological chemistry · February 2016
1,1,1-Trichloro-2,2-bis(p-chlorophenyl)ethane (DDT), the first organochlorine insecticide, and pyrethroid insecticides are sodium channel agonists. Although the use of DDT is banned in most of the world due to its detrimental impact on the ecosystem, indoo ...
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Journal ArticleInsect science · February 2016
Indoxacarb and metaflumizone belong to a relatively new class of sodium channel blocker insecticides (SCBIs). Due to intensive use of indoxacarb, field-evolved indoxacarb resistance has been reported in several lepidopteran pests, including the diamondback ...
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Journal ArticleInsect biochemistry and molecular biology · November 2015
In Drosophila melanogaster, the functions of voltage-gated sodium (Nav) channels are modulated by TipE and its orthologs. Here, we describe a novel TipE homolog of the American cockroach, Periplaneta americana, called PaTipE. Like DmTipE, PaTipE mRNAs are ...
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Journal ArticleInsect biochemistry and molecular biology · November 2015
Indoxacarb and metaflumizone are two sodium channel blocker insecticides (SCBIs). They preferably bind to and trap sodium channels in the slow-inactivated non-conducting state, a mode of action similar to that of local anesthetics (LAs). Recently, two sodi ...
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Journal ArticleMolecular pharmacology · August 2015
Voltage-gated sodium channels are the primary target of pyrethroid insecticides. Although it is well known that specific mutations in insect sodium channels confer knockdown resistance (kdr) to pyrethroids, the atomic mechanisms of pyrethroid-sodium channe ...
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Journal ArticlePesticide biochemistry and physiology · May 2015
It has been nearly three decades since the identification of the Drosophila Sodium Channel 1 (DSC1) gene from Drosophila melanogaster. The orthologs of the DSC1 gene have now been identified in other insect species including BSC1 from Blattella germanica. ...
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Journal ArticleInsect biochemistry and molecular biology · May 2015
The Drosophila melanogaster TipE protein is thought to be an insect sodium channel auxiliary subunit functionally analogous to the β subunits of mammalian sodium channels. Besides TipE, four TipE-homologous proteins (TEH1-4) have been identified. It has be ...
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Journal ArticleNeurotoxicology · March 2015
Voltage-gated sodium channels (Nav channels) are critical for electrical signaling in the nervous system and are the primary targets of the insecticides DDT and pyrethroids. In Drosophila melanogaster, besides the canonical Nav channel, Para (also called D ...
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Journal ArticleMolecular pharmacology · January 2015
Activation and inactivation of voltage-gated sodium channels are critical for proper electrical signaling in excitable cells. Pyrethroid insecticides promote activation and inhibit inactivation of sodium channels, resulting in prolonged opening of sodium c ...
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Chapter · January 1, 2015
Scorpion alpha and beta toxins interact with voltage-gated sodium channels (Navs) at two pharmacologically distinct sites. Alpha toxins bind at receptor site 3 and inhibit channel inactivation, whereas beta toxins bind at receptor site 4 and shi ...
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Journal ArticleInsect biochemistry and molecular biology · July 2014
Voltage-gated sodium channels are essential for the initiation and propagation of the action potential in neurons and other excitable cells. Because of their critical roles in electrical signaling, sodium channels are targets of a variety of naturally occu ...
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Journal ArticleNeuroscience · May 2014
Tetrodotoxin-sensitive persistent sodium currents, INaP, that activate at subthreshold voltages, have been detected in numerous vertebrate and invertebrate neurons. These currents are believed to be critical for regulating neuronal excitability. However, t ...
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Chapter · January 2014
Voltage-gated sodium channels are critical for the generation and propagation of action potentials. They are the primary target of several classes of insecticides, including DDT, pyrethroids and sodium channel blocker insecticides (SCBIs). DDT and pyrethro ...
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Journal ArticleNeurotoxicology · September 2013
Voltage-gated sodium channels are critical for electrical signaling in the nervous system. Pyrethroid insecticides exert their toxic action by modifying the gating of sodium channels. A valine to methionine mutation in the transmembrane segment 6 of domain ...
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Journal ArticleProceedings of the National Academy of Sciences of the United States of America · July 2013
Pyrethroid insecticides are widely used as one of the most effective control measures in the global fight against agricultural arthropod pests and mosquito-borne diseases, including malaria and dengue. They exert toxic effects by altering the function of v ...
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Journal ArticlePesticide biochemistry and physiology · July 2013
Pyrethroid insecticides target voltage-gated sodium channels, which are critical for electrical signaling in the nervous system. The intensive use of pyrethroids in controlling arthropod pests and disease vectors has led to many instances of pyrethroid res ...
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Journal ArticlePloS one · January 2013
β subunits of mammalian sodium channels play important roles in modulating the expression and gating of mammalian sodium channels. However, there are no orthologs of β subunits in insects. Instead, an unrelated protein, TipE in Drosophila melanogaster and ...
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Journal ArticlePloS one · January 2013
Insect voltage-gated sodium (Nav) channels are formed by a well-known pore-forming α-subunit encoded by para-like gene and ancillary subunits related to TipE from the mutation "temperature-induced-paralysis locus E." The role of these ancillary subunits in ...
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Journal ArticlePLoS genetics · January 2013
Voltage-gated ion channels are essential for electrical signaling in neurons and other excitable cells. Among them, voltage-gated sodium and calcium channels are four-domain proteins, and ion selectivity is strongly influenced by a ring of amino acids in t ...
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Journal ArticleInsect biochemistry and molecular biology · May 2012
DSC1 and BSC1 are two founding members of a novel family of invertebrate voltage-gated cation channels with close structural and evolutionary relationships to voltage-gated sodium and calcium channels. In this study, we searched the published genome sequen ...
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Journal ArticlePloS one · January 2012
Target site insensitivity resulting from point mutations within the voltage-gated sodium channel of the insect nervous system is known to be of primary importance in the development of resistance to pyrethroid insecticides. This study shifts current resear ...
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Journal ArticleScientific reports · January 2012
A previous study identified 3 nonsynonymous and 6 synonymous mutations in the entire mosquito sodium channel of Culex quinquefasciatus, the prevalence of which were strongly correlated with levels of resistance and increased dramatically following insectic ...
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Journal ArticleMolecular pharmacology · September 2011
Batrachotoxin (BTX), a steroidal alkaloid, and pyrethroid insecticides bind to distinct but allosterically coupled receptor sites on voltage-gated sodium channels and cause persistent channel activation. BTX presumably binds in the inner pore, whereas pyre ...
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Journal ArticleInsect biochemistry and molecular biology · July 2011
Deltamethrin, a pyrethroid insecticide, and BTG 502, an alkylamide insecticide, target voltage-gated sodium channels. Deltamethrin binds to a unique receptor site and causes prolonged opening of sodium channels by inhibiting deactivation and inactivation. ...
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Journal ArticleInsect biochemistry and molecular biology · July 2011
Drosophila Sodium Channel 1 (DSC1) was predicted to encode a sodium channel based on a high sequence similarity with vertebrate and invertebrate sodium channel genes. However, BSC1, a DSC1 ortholog in Blattella germanica, was recently shown to encode a cat ...
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Journal ArticleThe Journal of biological chemistry · May 2011
Scorpion β-toxins bind to the extracellular regions of the voltage-sensing module of domain II and to the pore module of domain III in voltage-gated sodium channels and enhance channel activation by trapping and stabilizing the voltage sensor of domain II ...
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Journal ArticleThe Journal of biological chemistry · April 2011
Ion permeation through voltage-gated sodium channels is modulated by various drugs and toxins. The atomistic mechanisms of action of many toxins are poorly understood. A steroidal alkaloid batrachotoxin (BTX) causes persistent channel activation by inhibit ...
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Journal ArticleGenetics · February 2011
We report the identification of bang senseless (bss), a Drosophila melanogaster mutant exhibiting seizure-like behaviors, as an allele of the paralytic (para) voltage-gated Na(+) (Na(V)) channel gene. Mutants are more prone to seizure episodes than normal ...
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Journal ArticleInsect biochemistry and molecular biology · January 2011
Voltage-gated sodium channels are the primary target of pyrethroid insecticides. Numerous point mutations in sodium channel genes have been identified in pyrethroid-resistant insect species, and many have been confirmed to reduce or abolish sensitivity of ...
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Journal ArticleInsect biochemistry and molecular biology · January 2011
A new class of sodium channel blocker insecticides (SCBIs), which include indoxacarb, its active metabolite, DCJW, and metaflumizone, preferably block inactivated states of both insect and mammalian sodium channels in a manner similar to that by which loca ...
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Journal ArticleToxicology and applied pharmacology · August 2010
Voltage-gated sodium channels are the primary target of pyrethroids, an important class of synthetic insecticides. Pyrethroids bind to a distinct receptor site on sodium channels and prolong the open state by inhibiting channel deactivation and inactivatio ...
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Journal ArticlePesticide biochemistry and physiology · June 2010
Sodium channel blocker insecticides (SCBIs) are a relatively new class of insecticides, with a mechanism of action different from those of other classes of insecticides that target voltage-gated sodium channels. These compounds have no effect at hyperpolar ...
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Journal ArticleThe Journal of biological chemistry · December 2009
Tetrodotoxin (TTX) is a potent blocker of voltage-gated sodium channels, but not all sodium channels are equally sensitive to inhibition by TTX. The molecular basis of differential TTX sensitivity of mammalian sodium channels has been largely elucidated. I ...
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Journal ArticleJournal of virology · October 2009
A broad Gag-specific CD8(+) T-cell response is associated with effective control of adult human immunodeficiency virus (HIV) infection. The association of certain HLA class I molecules, such as HLA-B*57, -B*5801, and -B*8101, with immune control is linked ...
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Journal ArticleNeurotoxicology · July 2009
Sodium channel blocker insecticides (SCBIs), such as indoxacarb and metaflumizone, are a new class of insecticides with a mechanism of action different from those of other insecticides that target sodium channels. SCBIs block sodium channels in a manner si ...
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Journal ArticleThe Biochemical journal · April 2009
A phenylalanine residue (Phe1519) in the sixth transmembrane segment of domain III (IIIS6) of the cockroach BgNa(v) sodium channel is required for the binding and action of pyrethroids. However, whether or not other residues in IIIS6 participate in the act ...
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Journal ArticleInsect biochemistry and molecular biology · February 2009
The voltage-gated sodium channel mediates the rapid rising phase of action potentials in almost all excitable cells and is a molecular target of a variety of neurotoxins including pyrethroid insecticides. Most studies have focused on the expression of sodi ...
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Journal ArticleToxicology and applied pharmacology · January 2009
Pyrethroid insecticides are classified as type I or type II based on their distinct symptomology and effects on sodium channel gating. Structurally, type II pyrethroids possess an alpha-cyano group at the phenylbenzyl alcohol position, which is lacking in ...
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Journal ArticleNeurotoxicology · May 2008
The field of neurotoxicology needs to satisfy two opposing demands: the testing of a growing list of chemicals, and resource limitations and ethical concerns associated with testing using traditional mammalian species. National and international government ...
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Journal ArticleInsect biochemistry and molecular biology · May 2008
Extensive alternative splicing and RNA editing have been documented for the transcript of DmNa(V) (formerly para), the sole sodium channel gene in Drosophila melanogaster. However, the functional consequences of these post-transcriptional modifications are ...
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Journal ArticleBMC genomics · September 2007
BackgroundNicotinic acetylcholine receptors (nAChRs) mediate fast synaptic cholinergic transmission in the insect central nervous system. The insect nAChR is the molecular target of a class of insecticides, neonicotinoids. Like mammalian nAChRs, i ...
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Journal ArticleInvertebrate neuroscience : IN · March 2007
Voltage-gated sodium channels are essential for the generation and propagation of action potentials (i.e., electrical impulses) in excitable cells. Although most of our knowledge about sodium channels is derived from decades of studies of mammalian isoform ...
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Journal ArticleToxicon : official journal of the International Society on Toxinology · March 2007
Receptor site-3 on voltage-gated sodium channels is targeted by a variety of structurally distinct toxins from scorpions, sea anemones, and spiders whose typical action is the inhibition of sodium current inactivation. This site interacts allosterically wi ...
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Journal ArticleToxicon : official journal of the International Society on Toxinology · March 2007
Voltage-gated sodium channels are a major target for toxins and insecticides due to their central role in excitability, but due to the conservation of these channels in Animalia most insecticides do not distinguish between those of insects and mammals, the ...
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Journal ArticleInsect biochemistry and molecular biology · November 2006
Fluvalinate is a pyrethroid insecticide that is widely used in the control of the varroa mite (Varroa destructor), an ecto-parasite of the honeybee. Previously we identified four fluvalinate-resistance-associated mutations in the sodium channel gene of the ...
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Journal ArticleNeurotoxicology · March 2006
Indoxacarb (DPX-JW062) was recently developed as a new oxadiazine insecticide with high insecticidal activity and low mammalian toxicity. Previous studies showed that indoxacarb and its bioactive metabolite, N-decarbomethoxyllated JW062 (DCJW), block insec ...
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Journal ArticleInsect biochemistry and molecular biology · February 2006
In a previous study, we showed that two alternative exons (G1 and G2 encoding IIIS3-S4) were involved in the differential sensitivity of two cockroach sodium channel splice variants, BgNa(v)1-1 and BgNa(v)2-1 (previously called KD1 and KD2), to deltamethri ...
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Journal ArticleMolecular pharmacology · February 2005
The voltage-gated sodium channel is the primary target site of pyrethroids, which constitute a major class of insecticides used worldwide. Pyrethroids prolong the opening of sodium channels by inhibiting deactivation and inactivation. Despite numerous atte ...
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Journal ArticleProceedings of the National Academy of Sciences of the United States of America · August 2004
The persistent tetrodotoxin (TTX)-sensitive sodium current, detected in neurons of many regions of mammalian brains, is associated with many essential neuronal activities, including boosting of excitatory synaptic inputs, acceleration of firing rates, and ...
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Journal ArticleThe Journal of biological chemistry · July 2004
Sodium channels play an essential role in generating the action potential in eukaryotic cells, and their transcripts, especially those in insects, undergo extensive A-to-I RNA editing. The functional consequences of RNA editing of sodium channel transcript ...
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Journal ArticleNeuron · April 2004
BSC1, which was originally identified by its sequence similarity to voltage-gated Na(+) channels, encodes a functional voltage-gated cation channel whose properties differ significantly from Na(+) channels. BSC1 has slower kinetics of activation and inacti ...
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Journal ArticleInsect biochemistry and molecular biology · July 2003
Voltage-gated sodium channels are essential for the generation and propagation of action potentials in most excitable cells. They are the target sites of several classes of insecticides and acaricides. Isolation of full-length sodium channel cDNA is a crit ...
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Journal ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience · July 2002
Alternative splicing is a major mechanism by which potassium and calcium channels increase functional diversity in animals. Extensive alternative splicing of the para sodium channel gene and developmental regulation of alternative splicing have been report ...
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Journal ArticleInsect biochemistry and molecular biology · April 2002
Pyrethroid insecticide resistance due to reduced nerve sensitivity, known as knockdown resistance (kdr or kdr-type), is linked to multiple point mutations in the para-homologous sodium channel genes. Previously we demonstrated that two mutations (E434K and ...
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Journal ArticleInsect biochemistry and molecular biology · April 2002
Pyrethroid insecticides alter the normal gating of voltage-gated sodium channels in the nervous system. Three sodium channel mutations (E434K, C764R, L993F) were recently identified in pyrethroid resistant German cockroach populations. In this report, we s ...
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Journal ArticleJournal of Apicultural Research · January 1, 2002
Varroa (Varroa destructor) has recently become resistant to Apistan, a pyrethroid pesticide with tau-fluvalinate as its active ingredient. In many insect pests, resistance to pyrethroid insecticides is due to reduced target-site (sodium channel) sensitivit ...
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Journal ArticleInsect biochemistry and molecular biology · April 2001
Voltage-gated sodium channels are integral transmembrane proteins responsible for the rapidly-rising phase of action potentials in most excitable cells. In mammals, the functional diversity and wide distribution of sodium channel proteins in various tissue ...
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Journal ArticleInsect biochemistry and molecular biology · October 2000
Knockdown resistance (kdr) to pyrethroid insecticides has been attributed to point mutations in the para sodium channel gene in more than a half dozen insect pest species. In this study, we identified two novel para mutations in five highly resistant kdr-t ...
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Journal ArticlePesticide Biochemistry and Physiology · January 1, 2000
Cypermethrin resistance level and mechanisms responsible for the resistance were investigated in a strain (Aves) of German cockroach, Blattella germanica (L.), collected recently from a Gainesville, Florida residence. Topical bioassay data revealed that th ...
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Journal ArticlePesticide Biochemistry and Physiology · August 1, 1998
A point mutation in the para-homologous sodium channel gene has been shown to be associated with knockdown resistance (kdr) in several insect species including the German cockroach. In this study, we analyzed the genomic organization of the region where th ...
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Journal ArticleInsect biochemistry and molecular biology · February 1997
Previous genetic and pharmacological studies suggest that knockdown-resistance (kdr) to pyrethroid insecticides likely results from a mutation(s) in the para sodium channel gene. In this study, para sodium channel genes from an insecticide-susceptible Germ ...
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Journal ArticleArchives of Insect Biochemistry and Physiology · January 1, 1996
Previous studies have shown that juvenile hormone esterase (JHE) activity and arylphorin titer were dramatically reduced in the hemolymph of Heliothis virescens larvae parasitized by Microplitis croceipes. Similar changes were observed in calyx fluid-injec ...
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Journal ArticleComparative biochemistry and physiology. Part B, Biochemistry & molecular biology · October 1994
The phenomenon of knockdown resistance (kdr) was first noted in the housefly (Musca domestica), and has subsequently be found (i.e. kdr-type resistance) in several other insect pests including the German cockroach (Blattella germanica). This type of resist ...
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Journal ArticleInsect biochemistry and molecular biology · July 1994
Pyrethroids are an important class of insecticides for controlling insect pests, including the German cockroach. Unfortunately, many insects have developed resistance to pyrethroids. One of the most important mechanisms of resistance is kdr (knockdown resi ...
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Journal ArticlePesticide Biochemistry and Physiology · January 1, 1993
Synaptosomal binding of [3H]batrachotoxinin A-20-α-benzoate ([3H]BTX-B), a potent sodium channel toxin, was measured in kdr-type resistant (Ectiban-R) and susceptible (CSMA) German cockroaches. Previous studies indicated that the Ectiban-R strain was 8.7-f ...
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Journal ArticleMedical and veterinary entomology · July 1992
Of fifteen compounds tested as synergists for chlorpyrifos against susceptible and resistant strains of Blattella germanica, the German cockroach, eleven were active against the resistant strain but only seven were synergistic against the susceptible strai ...
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Journal ArticlePesticide Biochemistry and Physiology · January 1, 1991
The biochemistry and genetics of kdr-type resistance in the Ectiban-R strain of German cockroach were studied to provide information on the molecular basis of this resistance and to allow for more detailed comparison to the well-studied kdr mechanism in ho ...
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Journal ArticleEnvironmental Entomology · December 1, 1990
Previously, we examined the effect of insecticides on four species of pteromalid parasitoids and their host, the house fly, Musca domestica L. Generally, the parasitoids are more susceptible to insecticides than the flies. In this study we examined the eff ...
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