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New page: left|200px<br /><applet load="1pb8" size="450" color="white" frame="true" align="right" spinBox="true" caption="1pb8, resolution 1.45Å" /> '''CRYSTAL STRUCTURE OF...
 
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[[Image:1pb8.jpg|left|200px]]<br /><applet load="1pb8" size="450" color="white" frame="true" align="right" spinBox="true"
caption="1pb8, resolution 1.45&Aring;" />
'''CRYSTAL STRUCTURE OF THE NR1 LIGAND BINDING CORE IN COMPLEX WITH D-SERINE AT 1.45 ANGSTROMS RESOLUTION'''<br />


==Overview==
==CRYSTAL STRUCTURE OF THE NR1 LIGAND BINDING CORE IN COMPLEX WITH D-SERINE AT 1.45 ANGSTROMS RESOLUTION==
Excitatory neurotransmission mediated by the N-methyl-D-aspartate subtype, of ionotropic glutamate receptors is fundamental to the development and, function of the mammalian central nervous system. NMDA receptors require, both glycine and glutamate for activation with NR1 and NR2 forming glycine, and glutamate sites, respectively. Mechanisms to describe agonist and, antagonist binding, and activation and desensitization of NMDA receptors, have been hampered by the lack of high-resolution structures. Here, we, describe the cocrystal structures of the NR1 S1S2 ligand-binding core with, the agonists glycine and D-serine (DS), the partial agonist D-cycloserine, (DCS) and the antagonist 5,7-dichlorokynurenic acid (DCKA). The cleft of, the S1S2 'clamshell' is open in the presence of the antagonist DCKA and, closed in the glycine, DS and DCS complexes. In addition, the NR1 S1S2, structure reveals the fold and interactions of loop 1, a cysteine-rich, region implicated in intersubunit allostery.
<StructureSection load='1pb8' size='340' side='right'caption='[[1pb8]], [[Resolution|resolution]] 1.45&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[1pb8]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1PB8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1PB8 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]] 1.45&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DSN:D-SERINE'>DSN</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=1pb8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1pb8 OCA], [https://pdbe.org/1pb8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1pb8 RCSB], [https://www.ebi.ac.uk/pdbsum/1pb8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1pb8 ProSAT]</span></td></tr>
</table>
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
  <jmolCheckbox>
    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/pb/1pb8_consurf.spt"</scriptWhenChecked>
    <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.spt</scriptWhenUnchecked>
    <text>to colour the structure by Evolutionary Conservation</text>
  </jmolCheckbox>
</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1pb8 ConSurf].
<div style="clear:both"></div>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Excitatory neurotransmission mediated by the N-methyl-D-aspartate subtype of ionotropic glutamate receptors is fundamental to the development and function of the mammalian central nervous system. NMDA receptors require both glycine and glutamate for activation with NR1 and NR2 forming glycine and glutamate sites, respectively. Mechanisms to describe agonist and antagonist binding, and activation and desensitization of NMDA receptors have been hampered by the lack of high-resolution structures. Here, we describe the cocrystal structures of the NR1 S1S2 ligand-binding core with the agonists glycine and D-serine (DS), the partial agonist D-cycloserine (DCS) and the antagonist 5,7-dichlorokynurenic acid (DCKA). The cleft of the S1S2 'clamshell' is open in the presence of the antagonist DCKA and closed in the glycine, DS and DCS complexes. In addition, the NR1 S1S2 structure reveals the fold and interactions of loop 1, a cysteine-rich region implicated in intersubunit allostery.


==About this Structure==
Mechanisms of activation, inhibition and specificity: crystal structures of the NMDA receptor NR1 ligand-binding core.,Furukawa H, Gouaux E EMBO J. 2003 Jun 16;22(12):2873-85. PMID:12805203<ref>PMID:12805203</ref>
1PB8 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with DSN as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1PB8 OCA].


==Reference==
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
Mechanisms of activation, inhibition and specificity: crystal structures of the NMDA receptor NR1 ligand-binding core., Furukawa H, Gouaux E, EMBO J. 2003 Jun 16;22(12):2873-85. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=12805203 12805203]
</div>
<div class="pdbe-citations 1pb8" style="background-color:#fffaf0;"></div>
 
==See Also==
*[[Glutamate receptor 3D structures|Glutamate receptor 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Large Structures]]
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
[[Category: Single protein]]
[[Category: Furukawa H]]
[[Category: Furukawa, H.]]
[[Category: Gouaux E]]
[[Category: Gouaux, E.]]
[[Category: DSN]]
[[Category: ligand binding receptor; rat; nr1]]
 
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Nov 20 23:39:24 2007''

Latest revision as of 00:21, 21 November 2024

CRYSTAL STRUCTURE OF THE NR1 LIGAND BINDING CORE IN COMPLEX WITH D-SERINE AT 1.45 ANGSTROMS RESOLUTION

1pb8, resolution 1.45Å

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