9SHE

Structure of the honeybee GABAA RDL receptor with GABA and Abamectin

これはPDB形式変換不可エントリーです。

9SHE の概要

• エントリーDOI: 10.2210/pdb9she/pdb
• EMDBエントリー: 54897
• 分子名称: Gamma-aminobutyric acid receptor subunit beta, GAMMA-AMINO-BUTANOIC ACID, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... (4 entities in total)
• 機能のキーワード: gabaa receptor, insect, neurotransmission, insecticides, membrane protein
• 由来する生物種: Apis mellifera (honey bee)
• タンパク質・核酸の鎖数: 5
• 化学式量合計: 274680.29

構造登録者

Laboure, T.,Nury, H. (登録日: 2025-08-26, 公開日: 2026-02-18, 最終更新日: 2026-04-15)

主引用文献

Laboure, T.,Pandey, M.P.,Zarkadas, E.,Juillan-Binard, C.,Baud, D.,Neyton, J.,Cens, T.,Rousset, M.,Dehez, F.,Charnet, P.,Nury, H.
Structures of the honeybee GABA A RDL receptor illuminate allosteric modulation.
Neuron, 114:1234-, 2026

PubMed Abstract: 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.

PubMed: 41653930
DOI: 10.1016/j.neuron.2025.12.013

実験手法

ELECTRON MICROSCOPY (3.2 Å)