4u5c: Difference between revisions
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==Crystal structure of GluA2, con-ikot-ikot snail toxin, partial agonist FW and postitive modulator (R,R)-2b complex== | ==Crystal structure of GluA2, con-ikot-ikot snail toxin, partial agonist FW and postitive modulator (R,R)-2b complex== | ||
<StructureSection load='4u5c' size='340' side='right' caption='[[4u5c]], [[Resolution|resolution]] 3.69Å' scene=''> | <StructureSection load='4u5c' size='340' side='right' caption='[[4u5c]], [[Resolution|resolution]] 3.69Å' scene=''> | ||
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<table><tr><td colspan='2'>[[4u5c]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4U5C OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4U5C FirstGlance]. <br> | <table><tr><td colspan='2'>[[4u5c]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4U5C OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4U5C FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=FWD:2-AMINO-3-(5-FLUORO-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YL)-PROPIONIC+ACID'>FWD</scene>, <scene name='pdbligand=FWF:N,N-[BIPHENYL-4,4-DIYLDI(2R)PROPANE-2,1-DIYL]DIPROPANE-2-SULFONAMIDE'>FWF</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=FWD:2-AMINO-3-(5-FLUORO-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YL)-PROPIONIC+ACID'>FWD</scene>, <scene name='pdbligand=FWF:N,N-[BIPHENYL-4,4-DIYLDI(2R)PROPANE-2,1-DIYL]DIPROPANE-2-SULFONAMIDE'>FWF</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'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4u5c FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4u5c OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4u5c RCSB], [http://www.ebi.ac.uk/pdbsum/4u5c PDBsum]</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=4u5c FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4u5c OCA], [http://pdbe.org/4u5c PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4u5c RCSB], [http://www.ebi.ac.uk/pdbsum/4u5c PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4u5c ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
<div class="pdbe-citations 4u5c" style="background-color:#fffaf0;"></div> | |||
==See Also== | |||
*[[Ionotropic Glutamate Receptors|Ionotropic Glutamate Receptors]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
Revision as of 00:59, 6 August 2016
Crystal structure of GluA2, con-ikot-ikot snail toxin, partial agonist FW and postitive modulator (R,R)-2b complexCrystal structure of GluA2, con-ikot-ikot snail toxin, partial agonist FW and postitive modulator (R,R)-2b complex
Structural highlights
Function[GRIA2_RAT] Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate.[1] [2] [3] [4] [5] [6] [7] [8] [9] [10] [11] [12] [13] [14] Publication Abstract from PubMedAMPA-sensitive glutamate receptors are crucial to the structural and dynamical properties of the brain, to the development and function of the central nervous system, and to the treatment of neurological conditions from depression to cognitive impairment. However, the molecular principles underlying AMPA receptor activation have remained elusive. Here, we determine multiple x-ray crystal structures of the GluA2 AMPA receptor in complex with a Conus striatus cone snail toxin, a positive allosteric modulator, and orthosteric agonists, at 3.8 to 4.1 angstrom resolution. We show how the toxin acts like a "straight jacket" on the ligand-binding domain (LBD) "gating ring," restraining the domains via both intra- and interdimer cross-links such that agonist-induced closure of the LBD "clamshells" is transduced into an irislike expansion of the gating ring. By structural analysis of activation-enhancing mutants, we show how the expansion of the LBD gating ring results in "pulling" forces on the M3 helices that, in turn, are coupled to ion channel gating. X-ray structures of AMPA receptor-cone snail toxin complexes illuminate activation mechanism.,Chen L, Duerr KL, Gouaux E Science. 2014 Aug 7. pii: 1258409. PMID:25103405[15] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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