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Proc Natl Acad Sci U S A
2017 Dec 05;11449:12922-12927. doi: 10.1073/pnas.1711699114.
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Molecular basis of selective resistance of the bumblebee BiNav1 sodium channel to tau-fluvalinate.
Wu S, Nomura Y, Du Y, Zhorov BS, Dong K.
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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 insecticides is a major mission of modern toxicology and pest management. Pyrethroids exert their toxic action by acting on insect voltage-gated sodium channels. Honeybees and bumblebees are highly sensitive to most pyrethroids, but are resistant to a particular pyrethroid, tau-fluvalinate (τ-FVL). Because of its unique selectivity, τ-FVL is widely used to control not only agricultural pests but also varroa mites, the principal ectoparasite of honeybees. However, the mechanism of bee resistance to τ-FVL largely remains elusive. In this study, we functionally characterized the sodium channel BiNav1-1 from the common eastern bumblebee (Bombus impatiens) in Xenopus oocytes and found that the BiNav1-1 channel is highly sensitive to six commonly used pyrethroids, but resistant to τ-FVL. Phylogenetic and mutational analyses revealed that three residues, which are conserved in sodium channels from 12 bee species, underlie resistance to τ-FVL or sensitivity to the other pyrethroids. Further computer modeling and mutagenesis uncovered four additional residues in the pyrethroid receptor sites that contribute to the unique selectivity of the bumblebee sodium channel to τ-FVL versus other pyrethroids. Our data contribute to understanding a long-standing enigma of selective pyrethroid toxicity in bees and may be used to guide future modification of pyrethroids to achieve highly selective control of pests with minimal effects on nontarget organisms.
Arena,
A meta-analysis comparing the sensitivity of bees to pesticides.
2014, Pubmed
Arena,
A meta-analysis comparing the sensitivity of bees to pesticides.
2014,
Pubmed Cameron,
Patterns of widespread decline in North American bumble bees.
2011,
Pubmed Casida,
Neuroactive insecticides: targets, selectivity, resistance, and secondary effects.
2013,
Pubmed Chakrabartty,
Helix propensities of the amino acids measured in alanine-based peptides without helix-stabilizing side-chain interactions.
1994,
Pubmed Cresswell,
Differential sensitivity of honey bees and bumble bees to a dietary insecticide (imidacloprid).
2012,
Pubmed Dong,
Molecular biology of insect sodium channels and pyrethroid resistance.
2014,
Pubmed Du,
Molecular evidence for dual pyrethroid-receptor sites on a mosquito sodium channel.
2013,
Pubmed
,
Xenbase Du,
Rotational Symmetry of Two Pyrethroid Receptor Sites in the Mosquito Sodium Channel.
2015,
Pubmed Du,
Identification of new batrachotoxin-sensing residues in segment IIIS6 of the sodium channel.
2011,
Pubmed
,
Xenbase Du,
A negative charge in transmembrane segment 1 of domain II of the cockroach sodium channel is critical for channel gating and action of pyrethroid insecticides.
2010,
Pubmed Garden,
Docking flexible ligands in proteins with a solvent exposure- and distance-dependent dielectric function.
2010,
Pubmed Goulson,
Decline and conservation of bumble bees.
2008,
Pubmed Kadala,
Pyrethroids differentially alter voltage-gated sodium channels from the honeybee central olfactory neurons.
2014,
Pubmed Kadala,
A use-dependent sodium current modification induced by type I pyrethroid insecticides in honeybee antennal olfactory receptor neurons.
2011,
Pubmed Katagiri,
Diastereoselectivity controlled by electrostatic repulsion between the negative charge on a trifluoromethyl group and that on aromatic rings.
2001,
Pubmed Kerr,
CLIMATE CHANGE. Climate change impacts on bumblebees converge across continents.
2015,
Pubmed Lenaeus,
Structures of closed and open states of a voltage-gated sodium channel.
2017,
Pubmed Long,
Crystal structure of a mammalian voltage-dependent Shaker family K+ channel.
2005,
Pubmed Lund,
Dose-dependent interaction of the pyrethroid isomers with sodium channels of squid axon membranes.
1982,
Pubmed Matter,
Evidence for C-Cl/C-Br...pi interactions as an important contribution to protein-ligand binding affinity.
2009,
Pubmed Oldroyd,
What's killing American honey bees?
2007,
Pubmed O'Reilly,
Modelling insecticide-binding sites in the voltage-gated sodium channel.
2006,
Pubmed Rinkevich,
Genetics, Synergists, and Age Affect Insecticide Sensitivity of the Honey Bee, Apis mellifera.
2015,
Pubmed Sanchez-Bayo,
Pesticide residues and bees--a risk assessment.
2014,
Pubmed Shen,
Structure of a eukaryotic voltage-gated sodium channel at near-atomic resolution.
2017,
Pubmed Sterk,
NEW INSIGHTS OF SIDE-EFFECTS OF TAU-FLUVALINATE ON BIOLOGICAL AGENTS AND POLLINATORS.
2015,
Pubmed Sula,
The complete structure of an activated open sodium channel.
2017,
Pubmed Tatebayashi,
Differential mechanism of action of the pyrethroid tetramethrin on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels.
1994,
Pubmed Tikhonov,
Mechanism of sodium channel block by local anesthetics, antiarrhythmics, and anticonvulsants.
2017,
Pubmed Vais,
Mutations of the para sodium channel of Drosophila melanogaster identify putative binding sites for pyrethroids.
2003,
Pubmed
,
Xenbase Warmke,
Functional expression of Drosophila para sodium channels. Modulation by the membrane protein TipE and toxin pharmacology.
1997,
Pubmed
,
Xenbase Wrzesińska,
A survey of pyrethroid-resistant populations of Meligethes aeneus F. in Poland indicates the incidence of numerous substitutions in the pyrethroid target site of voltage-sensitive sodium channels in individual beetles.
2014,
Pubmed Zhorov,
Potassium, sodium, calcium and glutamate-gated channels: pore architecture and ligand action.
2004,
Pubmed
