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-Structure paper
| タイトル | Structures of the honeybee GABA RDL receptor illuminate allosteric modulation. |
|---|---|
| ジャーナル・号・ページ | Neuron, Year 2026 |
| 掲載日 | 2026年2月6日 |
著者 | Tatiana Labouré / Mayank Prakash Pandey / Eleftherios Zarkadas / Céline Juillan-Binard / Delphine Baud / Jacques Neyton / Thierry Cens / Matthieu Rousset / François Dehez / Pierre Charnet / Hugues Nury / ![]() |
| PubMed 要旨 | A large share of insecticides targets insect ion channels. In particular, the GABA RDL (resistant to dieldrin) receptor is targeted by old pore blockers or more recent allosteric modulators binding ...A large share of insecticides targets insect ion channels. In particular, the GABA RDL (resistant to dieldrin) receptor is targeted by old pore blockers or more recent allosteric modulators binding to a cavity of its transmembrane domain. Here, we describe three ligand-binding sites and the associated receptor conformations, using a combination of cryoelectron microscopy (cryo-EM), electrophysiology, and molecular dynamics. The GABA site geometry is well conserved with that of mammalian receptors, in line with the absence of orthosteric insecticide. The transmembrane modulation site, occupied here by abamectin, exists in a closed-pore conformation. We identify a second allosteric transmembrane site using a compound named chrodrimanin B. Structures also reveal the existence of a conformation-dependent PIP lipid site. We anticipate our results to be the starting point for investigations on the physiological modulation of insect GABA receptors. The honeybee receptor structures may also foster the search for species-specific, environmentally benign insecticides. |
リンク | Neuron / PubMed:41653930 |
| 手法 | EM (単粒子) |
| 解像度 | 2.56 - 3.2 Å |
| 構造データ | EMDB-54897, PDB-9she: EMDB-54906, PDB-9sho: EMDB-54929, PDB-9sio: EMDB-54930, PDB-9siq: |
| 化合物 | ![]() ChemComp-ABU: ![]() ChemComp-NAG: ![]() PDB-1jnz: ![]() ChemComp-PT5: ![]() PDB-1jn7: |
| 由来 |
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キーワード | MEMBRANE PROTEIN / GABAA receptor / insect / neurotransmission / insecticides |
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