ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2011
Two amino acid residues contribute to a cation-π binding interaction in the binding site of an insect GABA receptor.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 40 citations in OpenAlex.
- Decoding the structural and functional diversity of GABAFrontiers in pharmacology · 2025Review
- Article
- Towards the Idea of Molecular Brains.International journal of molecular sciences · 2021Review
- Cation-π Interactions and their Functional Roles in Membrane Proteins.Journal of molecular biology · 2021Review
- A Single Mutation in the Outer Lipid-Facing Helix of a Pentameric Ligand-Gated Ion Channel Affects Channel Function Through a Radially-Propagating Mechanism.Frontiers in molecular biosciences · 2021Article
- Molecular basis for convergent evolution of glutamate recognition by pentameric ligand-gated ion channels.Scientific reports · 2015Article
- Incorporation of Non-Canonical Amino Acids.Advances in experimental medicine and biology · 2015Review
- Article
- Functional probes of drug-receptor interactions implicated by structural studies: Cys-loop receptors provide a fertile testing ground.Journal of medicinal chemistry · 2014Review
- 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
- Principles of agonist recognition in Cys-loop receptors.Frontiers in physiology · 2014Review
- Multiple tyrosine residues at the GABA binding pocket influence surface expression and mediate kinetics of the GABAA receptor.Journal of neurochemistry · 2013Article
- Crystal structures of the Helicobacter pylori MTAN enzyme reveal specific interactions between S-adenosylhomocysteine and the 5'-alkylthio binding subsite.Biochemistry · 2012Article
- GABA binding to an insect GABA receptor: a molecular dynamics and mutagenesis study.Biophysical journal · 2012Article
- Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines.Proceedings of the National Academy of Sciences of the United States of America · 2012Article
- Nematode cys-loop GABA receptors: biological function, pharmacology and sites of action for anthelmintics.Invertebrate neuroscience : IN · 2012Review
- Multiple Tyrosine Residues Contribute to GABA Binding in the GABA(C) Receptor Binding Pocket.ACS chemical neuroscience · 2012Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
Abstract
Cys-loop receptor binding sites characteristically possess an "aromatic box," where several aromatic amino acid residues surround the bound ligand. A cation-π interaction between one of these residues and the natural agonist is common, although the residue type and location are not conserved. Even in the closely related vertebrate GABA(A) and GABA(C) receptors, residues in distinct locations perform this role: in GABA(A) receptors, a Tyr residue in loop A forms a cation-π interaction with GABA, while in GABA(C) receptors it is a loop B residue. GABA-activated Cys-loop receptors also exist in invertebrates, where they have distinct pharmacologies and are the target of a range of pesticides. Here we examine the location of GABA in an insect binding site by incorporating a series of fluorinated Phe derivatives into the receptor binding pocket using unnatural amino acid mutagenesis, and evaluating the resulting receptors when expressed in Xenopus oocytes. A homology model suggests that two aromatic residues (in loops B and C) are positioned such that they could contribute to a cation-π interaction with the primary ammonium of GABA, and the data reveal a clear correlation between the GABA EC(50) and the cation-π binding ability both at Phe206 (loop B) and Tyr254 (loop C), demonstrating for the first time the contribution of two aromatic residues to a cation-π interaction in a Cys-loop receptor.
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What OpenQuestion holds
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.