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| | ==Crystal structure of the Drosophila GluR1A ligand binding domain complex with glutamate== | | ==Crystal structure of the Drosophila GluR1A ligand binding domain complex with glutamate== |
| - | <StructureSection load='5dt6' size='340' side='right' caption='[[5dt6]], [[Resolution|resolution]] 1.60Å' scene=''> | + | <StructureSection load='5dt6' size='340' side='right'caption='[[5dt6]], [[Resolution|resolution]] 1.60Å' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[5dt6]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Drome Drome]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5DT6 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5DT6 FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[5dt6]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Drosophila_melanogaster Drosophila melanogaster]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5DT6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5DT6 FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.598Å</td></tr> |
| - | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5dtb|5dtb]]</td></tr> | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr> |
| - | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">GluRIA, Glu-RI, CG8442 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=7227 DROME])</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=5dt6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5dt6 OCA], [https://pdbe.org/5dt6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5dt6 RCSB], [https://www.ebi.ac.uk/pdbsum/5dt6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5dt6 ProSAT]</span></td></tr> |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5dt6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5dt6 OCA], [http://pdbe.org/5dt6 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5dt6 RCSB], [http://www.ebi.ac.uk/pdbsum/5dt6 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5dt6 ProSAT]</span></td></tr> | + | |
| | </table> | | </table> |
| | == Function == | | == Function == |
| - | [[http://www.uniprot.org/uniprot/GLR1_DROME GLR1_DROME]] Receptor for glutamate. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. The postsynaptic actions of Glu are mediated by a variety of receptors that are named according to their selective agonists (By similarity). Forms ligand-gated ion channels which are activated by kainate.<ref>PMID:1359540</ref> | + | [https://www.uniprot.org/uniprot/GLR1_DROME GLR1_DROME] Receptor for glutamate. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. The postsynaptic actions of Glu are mediated by a variety of receptors that are named according to their selective agonists (By similarity). Forms ligand-gated ion channels which are activated by kainate.<ref>PMID:1359540</ref> |
| | <div style="background-color:#fffaf0;"> | | <div style="background-color:#fffaf0;"> |
| | == Publication Abstract from PubMed == | | == Publication Abstract from PubMed == |
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| | </div> | | </div> |
| | <div class="pdbe-citations 5dt6" style="background-color:#fffaf0;"></div> | | <div class="pdbe-citations 5dt6" style="background-color:#fffaf0;"></div> |
| | + | |
| | + | ==See Also== |
| | + | *[[Glutamate receptor 3D structures|Glutamate receptor 3D structures]] |
| | == References == | | == References == |
| | <references/> | | <references/> |
| | __TOC__ | | __TOC__ |
| | </StructureSection> | | </StructureSection> |
| - | [[Category: Drome]] | + | [[Category: Drosophila melanogaster]] |
| - | [[Category: Dharkar, P]] | + | [[Category: Large Structures]] |
| - | [[Category: Mayer, M L]] | + | [[Category: Dharkar P]] |
| - | [[Category: Membrane protein]] | + | [[Category: Mayer ML]] |
| Structural highlights
Function
GLR1_DROME Receptor for glutamate. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. The postsynaptic actions of Glu are mediated by a variety of receptors that are named according to their selective agonists (By similarity). Forms ligand-gated ion channels which are activated by kainate.[1]
Publication Abstract from PubMed
Phylogenetic analysis reveals AMPA, kainate, and NMDA receptor families in insect genomes, suggesting conserved functional properties corresponding to their vertebrate counterparts. However, heterologous expression of the Drosophila kainate receptor DKaiR1D and the AMPA receptor DGluR1A revealed novel ligand selectivity at odds with the classification used for vertebrate glutamate receptor ion channels (iGluRs). DKaiR1D forms a rapidly activating and desensitizing receptor that is inhibited by both NMDA and the NMDA receptor antagonist AP5; crystallization of the KaiR1D ligand-binding domain reveals that these ligands stabilize open cleft conformations, explaining their action as antagonists. Surprisingly, the AMPA receptor DGluR1A shows weak activation by its namesake agonist AMPA and also by quisqualate. Crystallization of the DGluR1A ligand-binding domain reveals amino acid exchanges that interfere with binding of these ligands. The unexpected ligand-binding profiles of insect iGluRs allows classical tools to be used in novel approaches for the study of synaptic regulation. VIDEO ABSTRACT.
Novel Functional Properties of Drosophila CNS Glutamate Receptors.,Li Y, Dharkar P, Han TH, Serpe M, Lee CH, Mayer ML Neuron. 2016 Dec 7;92(5):1036-1048. doi: 10.1016/j.neuron.2016.10.058. Epub 2016 , Nov 23. PMID:27889096[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Ultsch A, Schuster CM, Laube B, Schloss P, Schmitt B, Betz H. Glutamate receptors of Drosophila melanogaster: cloning of a kainate-selective subunit expressed in the central nervous system. Proc Natl Acad Sci U S A. 1992 Nov 1;89(21):10484-8. PMID:1359540
- ↑ Li Y, Dharkar P, Han TH, Serpe M, Lee CH, Mayer ML. Novel Functional Properties of Drosophila CNS Glutamate Receptors. Neuron. 2016 Dec 7;92(5):1036-1048. doi: 10.1016/j.neuron.2016.10.058. Epub 2016 , Nov 23. PMID:27889096 doi:http://dx.doi.org/10.1016/j.neuron.2016.10.058
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