5u1y

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==Crystal structure of the ATP-gated P2X7 ion channel bound to allosteric antagonist GW791343==
==Crystal structure of the ATP-gated P2X7 ion channel bound to allosteric antagonist GW791343==
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<StructureSection load='5u1y' size='340' side='right' caption='[[5u1y]], [[Resolution|resolution]] 3.30&Aring;' scene=''>
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<StructureSection load='5u1y' size='340' side='right'caption='[[5u1y]], [[Resolution|resolution]] 3.30&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[5u1y]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5U1Y OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5U1Y FirstGlance]. <br>
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<table><tr><td colspan='2'>[[5u1y]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Ailuropoda_melanoleuca Ailuropoda melanoleuca]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5U1Y OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5U1Y FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=7RS:N~2~-(3,4-DIFLUOROPHENYL)-N-{2-METHYL-5-[(PIPERAZIN-1-YL)METHYL]PHENYL}GLYCINAMIDE'>7RS</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></td></tr>
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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]] 3.3&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5u1l|5u1l]], [[5u1u|5u1u]], [[5u1v|5u1v]], [[5u1w|5u1w]], [[5u1x|5u1x]], [[5u2h|5u2h]]</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=7RS:N~2~-(3,4-DIFLUOROPHENYL)-N-{2-METHYL-5-[(PIPERAZIN-1-YL)METHYL]PHENYL}GLYCINAMIDE'>7RS</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></td></tr>
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<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=5u1y FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5u1y OCA], [http://pdbe.org/5u1y PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5u1y RCSB], [http://www.ebi.ac.uk/pdbsum/5u1y PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5u1y ProSAT]</span></td></tr>
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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=5u1y FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5u1y OCA], [https://pdbe.org/5u1y PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5u1y RCSB], [https://www.ebi.ac.uk/pdbsum/5u1y PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5u1y ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/G1M6C4_AILME G1M6C4_AILME]] Receptor for ATP that acts as a ligand-gated ion channel.[RuleBase:RU000681]
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[https://www.uniprot.org/uniprot/G1M6C4_AILME G1M6C4_AILME] Receptor for ATP that acts as a ligand-gated ion channel.[RuleBase:RU000681]
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The P2X7 receptor is a non-selective cation channel activated by extracellular adenosine triphosphate (ATP). Chronic activation of P2X7 underlies many health problems such as pathologic pain, yet we lack effective antagonists due to poorly understood mechanisms of inhibition. Here we present crystal structures of a mammalian P2X7 receptor complexed with five structurally-unrelated antagonists. Unexpectedly, these drugs all bind to an allosteric site distinct from the ATP-binding pocket in a groove formed between two neighboring subunits. This novel drug-binding pocket accommodates a diversity of small molecules mainly through hydrophobic interactions. Functional assays propose that these compounds allosterically prevent narrowing of the drug-binding pocket and the turret-like architecture during channel opening, which is consistent with a site of action distal to the ATP-binding pocket. These novel mechanistic insights will facilitate the development of P2X7-specific drugs for treating human diseases.
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Structural basis for subtype-specific inhibition of the P2X7 receptor.,Karasawa A, Kawate T Elife. 2016 Dec 9;5. pii: e22153. doi: 10.7554/eLife.22153. PMID:27935479<ref>PMID:27935479</ref>
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==See Also==
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*[[Ion channels 3D structures|Ion channels 3D structures]]
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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 5u1y" style="background-color:#fffaf0;"></div>
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== References ==
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<references/>
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Karasawa, A]]
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[[Category: Ailuropoda melanoleuca]]
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[[Category: Kawate, T]]
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[[Category: Large Structures]]
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[[Category: Membrane protein]]
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[[Category: Karasawa A]]
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[[Category: Membrane protein: atp-gated ion channel: allosteric antagonist bound: closed state]]
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[[Category: Kawate T]]

Current revision

Crystal structure of the ATP-gated P2X7 ion channel bound to allosteric antagonist GW791343

PDB ID 5u1y

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