9she

Structure of the honeybee GABAA RDL receptor with GABA and Abamectin

spinqualitylabelsall models 9she, resolution 3.20Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 9she is a 5 chain structure with sequence from Apis mellifera. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: Electron Microscopy, Resolution 3.2Å Ligands: A1JNZ, ABU, NAG Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function A0A8U0Y4W2_APIME Publication Abstract from PubMed A large share of insecticides targets insect ion channels. In particular, the GABA(A) 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(2) lipid site. We anticipate our results to be the starting point for investigations on the physiological modulation of insect GABA(A) receptors. The honeybee receptor structures may also foster the search for species-specific, environmentally benign insecticides. Structures of the honeybee GABA(A) RDL receptor illuminate allosteric modulation.,Laboure T, Pandey MP, Zarkadas E, Juillan-Binard C, Baud D, Neyton J, Cens T, Rousset M, Dehez F, Charnet P, Nury H Neuron. 2026 Feb 6:S0896-6273(25)00940-7. doi: 10.1016/j.neuron.2025.12.013. PMID:41653930 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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