5b3j
From Proteopedia
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- | '''Unreleased structure''' | ||
- | + | ==Activation of NMDA receptors and the mechanism of inhibition by ifenprodil== | |
+ | <StructureSection load='5b3j' size='340' side='right'caption='[[5b3j]], [[Resolution|resolution]] 2.90Å' scene=''> | ||
+ | == Structural highlights == | ||
+ | <table><tr><td colspan='2'>[[5b3j]] is a 8 chain structure with sequence from [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus], [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] and [https://en.wikipedia.org/wiki/Xenopus_laevis Xenopus laevis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5B3J OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5B3J FirstGlance]. <br> | ||
+ | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.9Å</td></tr> | ||
+ | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NA:SODIUM+ION'>NA</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=5b3j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5b3j OCA], [https://pdbe.org/5b3j PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5b3j RCSB], [https://www.ebi.ac.uk/pdbsum/5b3j PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5b3j ProSAT]</span></td></tr> | ||
+ | </table> | ||
+ | == Function == | ||
+ | [https://www.uniprot.org/uniprot/NMDZ1_XENLA NMDZ1_XENLA] Component of NMDA receptor complexes that function as heterotetrameric, ligand-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Channel activation requires binding of the neurotransmitter glutamate to the epsilon subunit, glycine binding to the zeta subunit, plus membrane depolarization to eliminate channel inhibition by Mg(2+) (PubMed:16214956, PubMed:19524674, PubMed:21677647, PubMed:25008524, PubMed:26912815, PubMed:27135925, Ref.11, PubMed:28232581). Sensitivity to glutamate and channel kinetics depend on the subunit composition (Probable).<ref>PMID:16214956</ref> <ref>PMID:19524674</ref> <ref>PMID:21677647</ref> <ref>PMID:25008524</ref> <ref>PMID:26912815</ref> <ref>PMID:27135925</ref> <ref>PMID:28232581</ref> [PDB:5IOV] | ||
+ | <div style="background-color:#fffaf0;"> | ||
+ | == Publication Abstract from PubMed == | ||
+ | The physiology of N-methyl-d-aspartate (NMDA) receptors is fundamental to brain development and function. NMDA receptors are ionotropic glutamate receptors that function as heterotetramers composed mainly of GluN1 and GluN2 subunits. Activation of NMDA receptors requires binding of neurotransmitter agonists to a ligand-binding domain (LBD) and structural rearrangement of an amino-terminal domain (ATD). Recent crystal structures of GluN1-GluN2B NMDA receptors bound to agonists and an allosteric inhibitor, ifenprodil, represent the allosterically inhibited state. However, how the ATD and LBD move to activate the NMDA receptor ion channel remains unclear. Here we applied X-ray crystallography, single-particle electron cryomicroscopy and electrophysiology to rat NMDA receptors to show that, in the absence of ifenprodil, the bi-lobed structure of GluN2 ATD adopts an open conformation accompanied by rearrangement of the GluN1-GluN2 ATD heterodimeric interface, altering subunit orientation in the ATD and LBD and forming an active receptor conformation that gates the ion channel. | ||
- | + | Activation of NMDA receptors and the mechanism of inhibition by ifenprodil.,Tajima N, Karakas E, Grant T, Simorowski N, Diaz-Avalos R, Grigorieff N, Furukawa H Nature. 2016 May 2. doi: 10.1038/nature17679. PMID:27135925<ref>PMID:27135925</ref> | |
- | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
- | [[Category: | + | </div> |
- | [[Category: | + | <div class="pdbe-citations 5b3j" style="background-color:#fffaf0;"></div> |
- | [[Category: | + | |
- | [[Category: Diaz-Avalos | + | ==See Also== |
- | [[Category: Grant | + | *[[Glutamate receptor 3D structures|Glutamate receptor 3D structures]] |
- | [[Category: | + | == References == |
- | [[Category: Karakas | + | <references/> |
- | [[Category: | + | __TOC__ |
+ | </StructureSection> | ||
+ | [[Category: Large Structures]] | ||
+ | [[Category: Mus musculus]] | ||
+ | [[Category: Rattus norvegicus]] | ||
+ | [[Category: Xenopus laevis]] | ||
+ | [[Category: Diaz-Avalos R]] | ||
+ | [[Category: Furukawa H]] | ||
+ | [[Category: Grant T]] | ||
+ | [[Category: Grigorieff N]] | ||
+ | [[Category: Karakas E]] | ||
+ | [[Category: Simorowski N]] | ||
+ | [[Category: Tajima N]] |
Current revision
Activation of NMDA receptors and the mechanism of inhibition by ifenprodil
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