ArticleInsect biochemistry and molecular biology2014
An atypical residue in the pore of Varroa destructor GABA-activated RDL receptors affects picrotoxin block and thymol modulation.
Article in Insect biochemistry and molecular biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 24 citations in OpenAlex.
- Convergent resistance to GABA receptor neurotoxins through plant-insect coevolution.Nature ecology & evolution · 2023Article
- The final frontier: ecological and evolutionary dynamics of a global parasite invasion.Biology letters · 2023Review
- Use of Thymol inInsects · 2022Article
- Article
- Article
- Orthosteric and Allosteric Activation of Human 5-HTBiophysical journal · 2020Article
- Caenorhabditis elegans muscle Cys-loop receptors as novel targets of terpenoids with potential anthelmintic activity.PLoS neglected tropical diseases · 2019Article
- Multiple combinations of RDL subunits diversify the repertoire of GABA receptors in the honey bee parasiteThe Journal of biological chemistry · 2018Article
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
GABA-activated RDL receptors are the insect equivalent of mammalian GABAA receptors, and play a vital role in neurotransmission and insecticide action. Here we clone the pore lining M2 region of the Varroa mite RDL receptor and show that it has 4 atypical residues when compared to M2 regions of most other insects, including bees, which are the major host of Varroa mites. We create mutant Drosophila RDL receptors containing these substitutions and characterise their effects on function. Using two electrode voltage clamp electrophysiology we show that one substitution (T6'M) ablates picrotoxin inhibition and increases the potency of GABA. This mutation also alters the effect of thymol, which enhances both insect and mammalian GABA responses, and is widely used as a miticide. Thymol decreases the GABA EC50 of WT receptors, enhancing responses, but in T6'M-containing receptors it is inhibitory. The other 3 atypical residues have no major effects on either the GABA EC50, the picrotoxin potency or the effect of thymol. In conclusion we show that the RDL 6' residue is important for channel block, activation and modulation, and understanding its function also has the potential to prove useful in the design of Varroa-specific insecticidal agents.
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