9she: Difference between revisions
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==Structure of the honeybee GABAA RDL receptor with GABA and Abamectin== | |||
<StructureSection load='9she' size='340' side='right'caption='[[9she]], [[Resolution|resolution]] 3.20Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[9she]] is a 5 chain structure with sequence from [https://en.wikipedia.org/wiki/Apis_mellifera Apis mellifera]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=9SHE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=9SHE FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 3.2Å</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=A1JNZ:(1~{R},2~{R},3~{S},4~{S},6~{S},8~{R},10~{E},10~{R},12~{S},13~{S},21~{R},24~{S})-2-[(2~{S})-butan-2-yl]-12-[(2~{R},4~{S},5~{S},6~{S})-4-methoxy-5-[(2~{S},4~{S},5~{S},6~{S})-4-methoxy-6-methyl-5-oxidanyl-oxan-2-yl]oxy-6-methyl-oxan-2-yl]oxy-3,11,13,22-tetramethyl-21,24-bis(oxidanyl)spiro[2,3-dihydropyran-6,6-3,7,19-trioxatetracyclo[15.6.1.1^{4,8}.1^{20,24}]pentacosa-10,14,16,22-tetraene]-2-one'>A1JNZ</scene>, <scene name='pdbligand=ABU:GAMMA-AMINO-BUTANOIC+ACID'>ABU</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=9she FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=9she OCA], [https://pdbe.org/9she PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=9she RCSB], [https://www.ebi.ac.uk/pdbsum/9she PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=9she ProSAT]</span></td></tr> | |||
</table> | |||
== Function == | |||
[https://www.uniprot.org/uniprot/A0A8U0Y4W2_APIME A0A8U0Y4W2_APIME] | |||
<div style="background-color:#fffaf0;"> | |||
== 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<ref>PMID:41653930</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
[[Category: Laboure | <div class="pdbe-citations 9she" style="background-color:#fffaf0;"></div> | ||
[[Category: Nury | == References == | ||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Apis mellifera]] | |||
[[Category: Large Structures]] | |||
[[Category: Laboure T]] | |||
[[Category: Nury H]] | |||