ArticleBiophysical journal2012
GABA binding to an insect GABA receptor: a molecular dynamics and mutagenesis study.
Article in Biophysical journal, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 64 citations in OpenAlex.
- Article
- Dynamics and Interplay of the Binding Pockets in the Glycine Receptor.Journal of chemical information and modeling · 2025Article
- Preclinical data on morpholine (3,5-di-tertbutyl-4-hydroxyphenyl) methanone induced anxiolysis.Naunyn-Schmiedeberg's archives of pharmacology · 2023Article
- Structure-function Studies of GABA (A) Receptors and Related computer-aided Studies.Journal of molecular neuroscience : MN · 2023Review
- Characterization of aFrontiers in molecular neuroscience · 2023Article
- Understanding the function of the GABAergic system and its potential role in rheumatoid arthritis.Frontiers in immunology · 2023Review
- Structural insights into the interaction between gabazine (SR-95531) andJournal of pesticide science · 2022Article
- Article
- Insect RDL Receptor Models for Virtual Screening: Impact of the Template Conformational State in Pentameric Ligand-Gated Ion Channels.ACS omega · 2022Article
- Molecular and Functional Characterization of GABA Receptor Subunits GRD and LCCH3 from Human LouseMolecular pharmacology · 2021Article
- Agonist and antagonist properties of an insect GABA-gated chloride channel (RDL) are influenced by heterologous expression conditions.PloS one · 2021Article
- Heterogeneous expression of GABA receptor-like subunits LCCH3 and GRD reveals functional diversity of GABA receptors in the honeybee Apis mellifera.British journal of pharmacology · 2020Article
- Article
- Mutagenesis computer experiments in pentameric ligand-gated ion channels: the role of simulation tools with different resolution.Interface focus · 2019Review
- Amino acid substitutions in the human homomeric βThe Journal of biological chemistry · 2019Article
- Multiple combinations of RDL subunits diversify the repertoire of GABA receptors in the honey bee parasiteThe Journal of biological chemistry · 2018Article
- A mutational and molecular dynamics study of the cys-loop GABA receptor Hco-UNC-49 from Haemonchus contortus: Agonist recognition in the nematode GABA receptor family.International journal for parasitology. Drugs and drug resistance · 2018Article
- Molecular Targets for Components of Essential Oils in the Insect Nervous System-A Review.Molecules (Basel, Switzerland) · 2017Review
- Identification of the ADPR binding pocket in the NUDT9 homology domain of TRPM2.The Journal of general physiology · 2017Article
- Structural correlates of affinity in fetal versus adult endplate nicotinic receptors.Nature communications · 2016Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
Abstract
RDL receptors are GABA-activated inhibitory Cys-loop receptors found throughout the insect CNS. They are a key target for insecticides. Here, we characterize the GABA binding site in RDL receptors using computational and electrophysiological techniques. A homology model of the extracellular domain of RDL was generated and GABA docked into the binding site. Molecular dynamics simulations predicted critical GABA binding interactions with aromatic residues F206, Y254, and Y109 and hydrophilic residues E204, S176, R111, R166, S176, and T251. These residues were mutated, expressed in Xenopus oocytes, and their functions assessed using electrophysiology. The data support the binding mechanism provided by the simulations, which predict that GABA forms many interactions with binding site residues, the most significant of which are cation-π interactions with F206 and Y254, H-bonds with E204, S205, R111, S176, T251, and ionic interactions with R111 and E204. These findings clarify the roles of a range of residues in binding GABA in the RDL receptor, and also show that molecular dynamics simulations are a useful tool to identify specific interactions in Cys-loop receptors.
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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.