3pmv

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[[Image:3pmv.png|left|200px]]
 
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==Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator==
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The line below this paragraph, containing "STRUCTURE_3pmv", creates the "Structure Box" on the page.
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<StructureSection load='3pmv' size='340' side='right'caption='[[3pmv]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3pmv]] 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=3PMV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PMV FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.8&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=557:N-[(2S)-2-{4-[4-(HYDROXYMETHYL)-3-(TRIFLUOROMETHYL)-1H-PYRAZOL-1-YL]PHENYL}PROPYL]PROPANE-2-SULFONAMIDE'>557</scene>, <scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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{{STRUCTURE_3pmv| PDB=3pmv | SCENE= }}
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3pmv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pmv OCA], [https://pdbe.org/3pmv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3pmv RCSB], [https://www.ebi.ac.uk/pdbsum/3pmv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3pmv ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/GRIA2_RAT 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.<ref>PMID:9351977</ref> <ref>PMID:19265014</ref> <ref>PMID:21172611</ref> <ref>PMID:12501192</ref> <ref>PMID:12015593</ref> <ref>PMID:12872125</ref> <ref>PMID:12730367</ref> <ref>PMID:16192394</ref> <ref>PMID:15591246</ref> <ref>PMID:17018279</ref> <ref>PMID:16483599</ref> <ref>PMID:19946266</ref> <ref>PMID:21317873</ref> <ref>PMID:21846932</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Starting from compound 1, we utilized biostructural data to successfully evolve an existing series into a new chemotype with a promising overall profile, exemplified by 19.
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===Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator===
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Structure based evolution of a novel series of positive modulators of the AMPA receptor.,Jamieson C, Maclean JK, Brown CI, Campbell RA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L Bioorg Med Chem Lett. 2011 Jan 15;21(2):805-11. Epub 2010 Nov 25. PMID:21190850<ref>PMID:21190850</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 3pmv" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_21190850}}, adds the Publication Abstract to the page
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*[[Glutamate receptor 3D structures|Glutamate receptor 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 21190850 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_21190850}}
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__TOC__
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</StructureSection>
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==About this Structure==
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[[Category: Large Structures]]
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[[3pmv]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PMV OCA].
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==Reference==
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<ref group="xtra">PMID:21190850</ref><references group="xtra"/>
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[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Brown, C I.]]
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[[Category: Brown CI]]
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[[Category: Campbell, R A.]]
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[[Category: Campbell RA]]
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[[Category: Gillen, K J.]]
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[[Category: Gillen KJ]]
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[[Category: Gillespie, J.]]
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[[Category: Gillespie J]]
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[[Category: Jamieson, C.]]
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[[Category: Jamieson C]]
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[[Category: Kazemier, B.]]
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[[Category: Kazemier B]]
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[[Category: Kiczun, M.]]
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[[Category: Kiczun M]]
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[[Category: Lamont, Y.]]
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[[Category: Lamont Y]]
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[[Category: Lyons, A J.]]
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[[Category: Lyons AJ]]
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[[Category: Maclean, J K.F.]]
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[[Category: Maclean JKF]]
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[[Category: Moir, E M.]]
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[[Category: Moir EM]]
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[[Category: Morrow, J A.]]
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[[Category: Morrow JA]]
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[[Category: Pantling, J.]]
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[[Category: Pantling J]]
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[[Category: Rankovic, Z.]]
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[[Category: Rankovic Z]]
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[[Category: Smith, L.]]
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[[Category: Smith L]]

Current revision

Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator

PDB ID 3pmv

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