ArticleBiochemistry2010
Molecular characterization of agonists that bind to an insect GABA receptor.
Article in Biochemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 34 citations in OpenAlex.
- Contributions of γ-Aminobutyric Acid (GABA) Receptors for the Activities ofPlants (Basel, Switzerland) · 2024Article
- Prediction of the Neurotoxic Potential of Chemicals Based on Modelling of Molecular Initiating Events Upstream of the Adverse Outcome Pathways of (Developmental) Neurotoxicity.International journal of molecular sciences · 2022Article
- Agonist and antagonist properties of an insect GABA-gated chloride channel (RDL) are influenced by heterologous expression conditions.PloS one · 2021Article
- Stop the crop: Insights into the insecticidal mode of action of cinnamodial against mosquitoes.Pesticide biochemistry and physiology · 2021Article
- Mutagenesis computer experiments in pentameric ligand-gated ion channels: the role of simulation tools with different resolution.Interface focus · 2019Review
- Molecular Targets for Components of Essential Oils in the Insect Nervous System-A Review.Molecules (Basel, Switzerland) · 2017Review
- A molecular characterization of the agonist binding site of a nematode cys-loop GABA receptor.British journal of pharmacology · 2015Article
- Article
- An atypical residue in the pore of Varroa destructor GABA-activated RDL receptors affects picrotoxin block and thymol modulation.Insect biochemistry and molecular biology · 2014Article
- Article
- Insights into the binding of GABA to the insect RDL receptor from atomistic simulations: a comparison of models.Journal of computer-aided molecular design · 2014Article
- GABA binding to an insect GABA receptor: a molecular dynamics and mutagenesis study.Biophysical journal · 2012Article
- The pharmacological profile of ELIC, a prokaryotic GABA-gated receptor.Neuropharmacology · 2012Article
- Two amino acid residues contribute to a cation-π binding interaction in the binding site of an insect GABA receptor.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2011Article
- Probing structural features and binding mode of 3-arylpyrimidin-2,4-diones within housefly γ-aminobutyric acid (GABA) receptor.International journal of molecular sciences · 2011Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 2 countries.
Funding
Abstract
Ionotropic GABA receptors are widely distributed throughout the vertebrate and invertebrate central nervous system (CNS) where they mediate inhibitory neurotransmission. One of the most widely studied insect GABA receptors is constructed from RDL (resistance to dieldrin) subunits from Drosophila melanogaster. The aim of this study was to determine critical features of agonists binding to RDL receptors using in silico and experimental data. Partial atomic charges and dipole separation distances of a range of GABA analogues were calculated, and the potency of the analogues was determined using RDL receptors expressed in Xenopus oocytes. These data revealed functional agonists require an ammonium group and an acidic group with an optimum separation distance of approximately 5 A. To determine how the agonists bind to the receptor, a homology model of the extracellular domain was generated and agonists were docked into the binding site. The docking studies support the requirements for functional agonists and also revealed a range of potential interactions with binding site residues, including hydrogen bonds and cation-pi interactions. We conclude that the model and docking procedures yield a good model of the insect GABA receptor binding site and the location of agonists within it.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.