5u1w: Difference between revisions
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==Crystal structure of the ATP-gated P2X7 ion channel bound to allosteric antagonist AZ10606120== | ==Crystal structure of the ATP-gated P2X7 ion channel bound to allosteric antagonist AZ10606120== | ||
<StructureSection load='5u1w' size='340' side='right' caption='[[5u1w]], [[Resolution|resolution]] 3.50Å' scene=''> | <StructureSection load='5u1w' size='340' side='right'caption='[[5u1w]], [[Resolution|resolution]] 3.50Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[5u1w]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5U1W OCA]. For a <b>guided tour on the structure components</b> use [ | <table><tr><td colspan='2'>[[5u1w]] 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=5U1W OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5U1W FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=7RY:N-[2-({2-[(2-HYDROXYETHYL)AMINO]ETHYL}AMINO)QUINOLIN-5-YL]-2-[(3S,5S,7S)-TRICYCLO[3.3.1.1~3,7~]DECAN-1-YL]ACETAMIDE'>7RY</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene> | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.501Å</td></tr> | ||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=7RY:N-[2-({2-[(2-HYDROXYETHYL)AMINO]ETHYL}AMINO)QUINOLIN-5-YL]-2-[(3S,5S,7S)-TRICYCLO[3.3.1.1~3,7~]DECAN-1-YL]ACETAMIDE'>7RY</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'>[ | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5u1w FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5u1w OCA], [https://pdbe.org/5u1w PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5u1w RCSB], [https://www.ebi.ac.uk/pdbsum/5u1w PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5u1w ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
[ | [https://www.uniprot.org/uniprot/G1M6C4_AILME G1M6C4_AILME] Receptor for ATP that acts as a ligand-gated ion channel.[RuleBase:RU000681] | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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</div> | </div> | ||
<div class="pdbe-citations 5u1w" style="background-color:#fffaf0;"></div> | <div class="pdbe-citations 5u1w" style="background-color:#fffaf0;"></div> | ||
==See Also== | |||
*[[Ion channels 3D structures|Ion channels 3D structures]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Ailuropoda melanoleuca]] | ||
[[Category: | [[Category: Large Structures]] | ||
[[Category: | [[Category: Karasawa A]] | ||
[[Category: | [[Category: Kawate T]] | ||
Latest revision as of 15:13, 6 November 2024
Crystal structure of the ATP-gated P2X7 ion channel bound to allosteric antagonist AZ10606120Crystal structure of the ATP-gated P2X7 ion channel bound to allosteric antagonist AZ10606120
Structural highlights
FunctionG1M6C4_AILME Receptor for ATP that acts as a ligand-gated ion channel.[RuleBase:RU000681] Publication Abstract from PubMedThe 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. 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[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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