Cyclodiene Insecticide Resistance: From Molecular to Population Genetics

ffrench-Constant, Richard H.; Anthony, Nicola M.; Aronstein, Kate; Rocheleau, Thomas A.; Stilwell, Geoff

doi:10.1146/annurev.ento.45.1.449

Cited by 191 publications

(129 citation statements)

References 68 publications

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“…This associates sodium channel mutations with olfactory and chemotactic defects (Lilly and Carlson, 1990) and with changes in sexual behaviour (Tompkins et al, 1982(Tompkins et al, , 1983. In another unrelated point mutation conferring resistance to the cyclodienes, a mutation in the structural gene encoding the g-aminobutyric acid receptor (rdl or resistance to dieldrin) also appears to induce reversible temperaturesensitive paralysis (Ffrench-Constant et al, 2000).…”

Section: Discussionmentioning

confidence: 99%

Analogous pleiotropic effects of insecticide resistance genotypes in peach–potato aphids and houseflies

et al. 2003

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We show that single-point mutations conferring target-site resistance (kdr) to pyrethroids and DDT in aphids and houseflies, and gene amplification conferring metabolic resistance (carboxylesterase) to organophosphates and carbamates in aphids, can have deleterious pleiotropic effects on fitness. Behavioural studies on peach-potato aphids showed that a reduced response to alarm pheromone was associated with both gene amplification and the kdr target-site mutation. In this species, gene amplification was also associated with a decreased propensity to move from senescing leaves to fresh leaves at low temperature. Housefly genotypes possessing the identical kdr mutation were also shown to exhibit behavioural differences in comparison with susceptible insects. In this species, resistant individuals showed no positional preference along a temperature gradient while susceptible genotypes exhibited a strong preference for warmer temperatures.

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Section: Discussionmentioning

confidence: 99%

Analogous pleiotropic effects of insecticide resistance genotypes in peach–potato aphids and houseflies

et al. 2003

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“…The molecular localization of the NCA site defined here (Fig. 1B) was first indicated by mutagenesis studies (16) as A2Ј (17)(18)(19)(20), T6Ј (21,22), and L9Ј (23,24) in the cytoplasmic half of the transmembrane 2 domain of the channel (Fig. 2).…”

mentioning

confidence: 83%

Structural model for γ-aminobutyric acid receptor noncompetitive antagonist binding: Widely diverse structures fit the same site

Chen

Durkin

Casida

2006

Proc. Natl. Acad. Sci. U.S.A.

150

151

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Several major insecticides, including ␣-endosulfan, lindane, and fipronil, and the botanical picrotoxinin are noncompetitive antagonists (NCAs) for the GABA receptor. We showed earlier that human ␤3 homopentameric GABAA receptor recognizes all of the important GABAergic insecticides and reproduces the high insecticide sensitivity and structure-activity relationships of the native insect receptor. Despite large structural diversity, the NCAs are proposed to fit a single binding site in the chloride channel lumen lined by five transmembrane 2 segments. This hypothesis is examined with the ␤3 homopentamer by mutagenesis, pore structure studies, NCA binding, and molecular modeling. The 15 amino acids in the cytoplasmic half of the pore were mutated to cysteine, serine, or other residue for 22 mutants overall. Localization of A-1 C, A2 C, T6 C, and L9 C (index numbers for the transmembrane 2 region) in the channel lumen was established by disulfide cross-linking. Binding of two NCA radioligands ␤3 homopentamer ͉ transmembrane 2 ͉ insecticide ͉ disulfide trapping ͉ receptor model P est insect control in the past 60 years was achieved, in part, by application of Ͼ3 billion (3 ϫ 10 9 ) pounds of polychlorocycloalkane insecticides, including cyclodienes (e.g., ␣-endosulfan and dieldrin), lindane and its isomers, and others, which are now highly restricted or banned except for endosulfan and some uses of lindane (1-3). One of the replacement compounds is the phenylpyrazole fipronil. All of these insecticides and the botanical picrotoxinin (PTX) have widely diverse chemical structures but appear to act at the same nerve target. It is therefore important to understand how these compounds work in mammals and insects, or how they do not work when resistant insect strains appear.The GABA-gated chloride channel is the target for the insecticides and toxicants referred to above based on radioligand binding and electrophysiology studies (3)(4)(5)(6)(7)(8)(9)(10) (Fig. 1A). All of these compounds act in mammals and insects as noncompetitive antagonists (NCAs) to block chloride flux so the target is referred to as the GABA receptor NCA-binding site. Vertebrate GABA receptors consist of ␣, ␤, ␥, , and other subunits in various combinations, for example, ␣ 1 ␤ 2 ␥ 2 as a heteropentamer and 1 as a homopentamer (13-15). The molecular localization of the NCA site defined here (Fig. 1B) was first indicated by mutagenesis studies (16) as A2Ј (17-20), T6Ј (21, 22), and L9Ј (23, 24) in the cytoplasmic half of the transmembrane 2 domain of the channel (Fig. 2). Drosophila resistant to dieldrin (RDL) have a mutation conferring GABA receptor insensitivity identified as A2ЈS (17). The NCA target of the GABA A receptor requires a ␤ subunit, and a ␤ 3 homopentamer is sufficient for binding (9,26). Importantly, the ␤ 3 subunit from human brain, when expressed in insect Sf9 cells, assembles to form a receptor sensitive to all of the important GABAergic insecticides (9) and, surprisingly, reproduces the insecticide sensitivity and structureactivit...

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“…1) confers cyclodiene resistance in a broad range of insects. 6) In the b3 homopentameric channel, the 12 amino acids shown in Fig. 1 were mutated to Cys, Ser, or other residues.…”

Section: Three Amino Acids Important To Nca Insecticide Bindingmentioning

confidence: 99%

“…1) confers high insecticide resistance and low GABAR sensitivity 6) with varying degrees of cross resistance to diverse types of NCAs. The relative importance of the 2Ј, 6Ј and 9Ј sites in insecticide binding may contribute to differences in resistance levels, e.g.…”

Section: Resistance Mechanismsmentioning

confidence: 99%

Insecticide interactions with .GAMMA.-aminobutyric acid and nicotinic receptors: predictive aspects of structural models

Casida¹,

Tomizawa²

2008

J. Pestic. Sci.

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An insecticide binding site may be blocked by widely diverse chemicals, as with the g-aminobutyric acid receptor (GABAR), or accept only closely related compounds, as illustrated by the nicotinic acetylcholine (ACh) receptor (nAChR). The human GABAR b3-homopentamer resembles the insect receptor in sensitivity and specificity for noncompetitive antagonists (NCAs), prompting exhaustive site-directed mutagenesis (cysteine scanning), which pinpointed the critical active site as pore-facing residues Ala-2Ј, Thr-6Ј and Leu-9Ј and led to a binding site model which fits several classes of insecticidal NCAs. The nAChR agonist site was approached with an ACh binding protein (AChBP) by photoaffinity labeling and neonicotinoid docking. Chloropyridinyl chlorine contacts Ile-106/Met-116 and nitrogen is directed to Ile-118/Trp-147 via a solvent bridge(s). The guanidine/amidine plane undergoes p-stacking with Tyr-188, and the nitro/cyano pharmacophore interacts with Ser-189/Cys-190, thereby defining the binding pocket that models AChBP and possibly nAChR potency and selectivity.

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Cyclodiene Insecticide Resistance: From Molecular to Population Genetics

Cited by 191 publications

References 68 publications

Analogous pleiotropic effects of insecticide resistance genotypes in peach–potato aphids and houseflies

Analogous pleiotropic effects of insecticide resistance genotypes in peach–potato aphids and houseflies

Structural model for γ-aminobutyric acid receptor noncompetitive antagonist binding: Widely diverse structures fit the same site

Insecticide interactions with .GAMMA.-aminobutyric acid and nicotinic receptors: predictive aspects of structural models

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