3rey: Difference between revisions

Latest revision as of 17:16, 1 November 2023

Thermostabilised adenosine A2A receptor in complex with XAC

Structural highlights

3rey is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 3.309Å
Ligands:	XAC
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

AA2AR_HUMAN Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.

Publication Abstract from PubMed

Methylxanthines, including caffeine and theophylline, are among the most widely consumed stimulant drugs in the world. These effects are mediated primarily via blockade of adenosine receptors. Xanthine analogs with improved properties have been developed as potential treatments for diseases such as Parkinson's disease. Here we report the structures of a thermostabilized adenosine A(2A) receptor in complex with the xanthines xanthine amine congener and caffeine, as well as the A(2A) selective inverse agonist ZM241385. The receptor is crystallized in the inactive state conformation as defined by the presence of a salt bridge known as the ionic lock. The complete third intracellular loop, responsible for G protein coupling, is visible consisting of extended helices 5 and 6. The structures provide new insight into the features that define the ligand binding pocket of the adenosine receptor for ligands of diverse chemotypes as well as the cytoplasmic regions that interact with signal transduction proteins.

Structure of the adenosine A(2A) receptor in complex with ZM241385 and the xanthines XAC and caffeine.,Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH Structure. 2011 Sep 7;19(9):1283-93. PMID:21885291^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH. Structure of the adenosine A(2A) receptor in complex with ZM241385 and the xanthines XAC and caffeine. Structure. 2011 Sep 7;19(9):1283-93. PMID:21885291 doi:10.1016/j.str.2011.06.014

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OCA

[1] Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH. Structure of the adenosine A(2A) receptor in complex with ZM241385 and the xanthines XAC and caffeine. Structure. 2011 Sep 7;19(9):1283-93. PMID:21885291 doi:10.1016/j.str.2011.06.014

[1]

@@ Line 1: / Line 1: @@
 ==Thermostabilised adenosine A2A receptor in complex with XAC==
-<StructureSection load='3rey' size='340' side='right' caption='[[3rey]], [[Resolution|resolution]] 3.31&Aring;' scene=''>
+<StructureSection load='3rey' size='340' side='right'caption='[[3rey]], [[Resolution|resolution]] 3.31&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[3rey]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3REY OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3REY FirstGlance]. <br>
+<table><tr><td colspan='2'>[[3rey]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3REY OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3REY FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=XAC:N-(2-AMINOETHYL)-2-[4-(2,6-DIOXO-1,3-DIPROPYL-2,3,6,7-TETRAHYDRO-1H-PURIN-8-YL)PHENOXY]ACETAMIDE'>XAC</scene></td></tr>
+</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.309&#8491;</td></tr>
-<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3pwh|3pwh]], [[3rfm|3rfm]]</td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=XAC:N-(2-AMINOETHYL)-2-[4-(2,6-DIOXO-1,3-DIPROPYL-2,3,6,7-TETRAHYDRO-1H-PURIN-8-YL)PHENOXY]ACETAMIDE'>XAC</scene></td></tr>
-<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">ADORA2A ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</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=3rey FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rey OCA], [https://pdbe.org/3rey PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3rey RCSB], [https://www.ebi.ac.uk/pdbsum/3rey PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3rey ProSAT]</span></td></tr>
-<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=3rey FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rey OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rey RCSB], [http://www.ebi.ac.uk/pdbsum/3rey PDBsum]</span></td></tr>
 </table>
+== Function ==
+[https://www.uniprot.org/uniprot/AA2AR_HUMAN AA2AR_HUMAN] Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
 <div style="background-color:#fffaf0;">
 == Publication Abstract from PubMed ==
@@ Line 16: / Line 18: @@
 From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
 </div>
+<div class="pdbe-citations 3rey" style="background-color:#fffaf0;"></div>
 ==See Also==
-*[[Adenosine A2A receptor|Adenosine A2A receptor]]
+*[[Adenosine A2A receptor 3D structures|Adenosine A2A receptor 3D structures]]
-*[[G protein-coupled receptor|G protein-coupled receptor]]
 == References ==
 <references/>
@@ Line 25: / Line 27: @@
 </StructureSection>
 [[Category: Homo sapiens]]
-[[Category: Bennett, K]]
+[[Category: Large Structures]]
-[[Category: Congreve, M]]
+[[Category: Bennett K]]
-[[Category: Dore, A S]]
+[[Category: Congreve M]]
-[[Category: Errey, J C]]
+[[Category: Dore AS]]
-[[Category: Hollenstein, K]]
+[[Category: Errey JC]]
-[[Category: Hurrell, E]]
+[[Category: Hollenstein K]]
-[[Category: Magnani, F]]
+[[Category: Hurrell E]]
-[[Category: Marshall, F H]]
+[[Category: Magnani F]]
-[[Category: Ng, I]]
+[[Category: Marshall FH]]
-[[Category: Robertson, N]]
+[[Category: Ng I]]
-[[Category: Tate, C G]]
+[[Category: Robertson N]]
-[[Category: Tehan, B]]
+[[Category: Tate CG]]
-[[Category: Weir, M]]
+[[Category: Tehan B]]
-[[Category: G-protein]]
+[[Category: Weir M]]
-[[Category: Gpcr]]
-[[Category: Membrane protein]]
-[[Category: Signaling protein]]

3rey: Difference between revisions

Latest revision as of 17:16, 1 November 2023

Thermostabilised adenosine A2A receptor in complex with XAC

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

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