1mqh

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[[Image:1mqh.jpg|left|200px]]
 
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==Crystal Structure of the GluR2 Ligand Binding Core (S1S2J) in Complex with Bromo-Willardiine at 1.8 Angstroms Resolution==
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The line below this paragraph, containing "STRUCTURE_1mqh", creates the "Structure Box" on the page.
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<StructureSection load='1mqh' size='340' side='right'caption='[[1mqh]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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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'>[[1mqh]] 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=1MQH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1MQH FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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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=BWD:2-AMINO-3-(5-BROMO-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YL)-PROPIONIC+ACID'>BWD</scene></td></tr>
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{{STRUCTURE_1mqh| PDB=1mqh | 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=1mqh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mqh OCA], [https://pdbe.org/1mqh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1mqh RCSB], [https://www.ebi.ac.uk/pdbsum/1mqh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1mqh 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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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/mq/1mqh_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</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=1mqh ConSurf].
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<div style="clear:both"></div>
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'''Crystal Structure of the GluR2 Ligand Binding Core (S1S2J) in Complex with Bromo-Willardiine at 1.8 Angstroms Resolution'''
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==See Also==
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*[[Glutamate receptor 3D structures|Glutamate receptor 3D structures]]
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== References ==
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==Overview==
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<references/>
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An unresolved problem in understanding neurotransmitter receptor function concerns the mechanism(s) by which full and partial agonists elicit different amplitude responses at equal receptor occupancy. The widely held view of 'partial agonism' posits that resting and active states of the receptor are in equilibrium, and partial agonists simply do not shift the equilibrium toward the active state as efficaciously as full agonists. Here we report findings from crystallographic and electrophysiological studies of the mechanism of activation of an AMPA-subtype glutamate receptor ion channel. In these experiments, we used 5-substituted willardiines, a series of partial agonists that differ by only a single atom. Our results show that the GluR2 ligand-binding core can adopt a range of ligand-dependent conformational states, which in turn control the open probability of discrete subconductance states of the intact ion channel. Our findings thus provide a structure-based model of partial agonism.
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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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1MQH is a [[Single protein]] structure of 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=1MQH OCA].
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==Reference==
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Structural basis for partial agonist action at ionotropic glutamate receptors., Jin R, Banke TG, Mayer ML, Traynelis SF, Gouaux E, Nat Neurosci. 2003 Aug;6(8):803-10. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12872125 12872125]
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[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Single protein]]
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[[Category: Banke TG]]
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[[Category: Banke, T G.]]
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[[Category: Gouaux E]]
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[[Category: Gouaux, E.]]
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[[Category: Jin R]]
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[[Category: Jin, R.]]
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[[Category: Mayer ML]]
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[[Category: Mayer, M L.]]
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[[Category: Traynelis SF]]
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[[Category: Traynelis, S F.]]
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[[Category: Bromo-willardiine]]
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[[Category: Glur2]]
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[[Category: Ionotropic glutamate receptor]]
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[[Category: Ligand binding core]]
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[[Category: Partial agonist]]
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[[Category: S1s2]]
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[[Category: Willardiine]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 01:35:54 2008''
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Current revision

Crystal Structure of the GluR2 Ligand Binding Core (S1S2J) in Complex with Bromo-Willardiine at 1.8 Angstroms Resolution

PDB ID 1mqh

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