3uzc

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[[Image:3uzc.jpg|left|200px]]
 
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==Thermostabilised Adenosine A2A receptor in complex with 4-(3-amino-5-phenyl-1,2,4-triazin-6-yl)-2-chlorophenol==
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The line below this paragraph, containing "STRUCTURE_3uzc", creates the "Structure Box" on the page.
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<StructureSection load='3uzc' size='340' side='right'caption='[[3uzc]], [[Resolution|resolution]] 3.34&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'>[[3uzc]] 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=3UZC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3UZC 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]] 3.341&#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=T4E:4-(3-AMINO-5-PHENYL-1,2,4-TRIAZIN-6-YL)-2-CHLOROPHENOL'>T4E</scene></td></tr>
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{{STRUCTURE_3uzc| PDB=3uzc | 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=3uzc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3uzc OCA], [https://pdbe.org/3uzc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3uzc RCSB], [https://www.ebi.ac.uk/pdbsum/3uzc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3uzc ProSAT]</span></td></tr>
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</table>
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== Function ==
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[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.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Potent, ligand efficient, selective, and orally efficacious 1,2,4-triazine derivatives have been identified using structure based drug design approaches as antagonists of the adenosine A(2A) receptor. The X-ray crystal structures of compounds 4e and 4g bound to the GPCR illustrate that the molecules bind deeply inside the orthosteric binding cavity. In vivo pharmacokinetic and efficacy data for compound 4k are presented, demonstrating the potential of this series of compounds for the treatment of Parkinson's disease.
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===Thermostabilised Adenosine A2A receptor in complex with 4-(3-amino-5-phenyl-1,2,4-triazin-6-yl)-2-chlorophenol===
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Discovery of 1,2,4-Triazine Derivatives as Adenosine A(2A) Antagonists using Structure Based Drug Design.,Congreve M, Andrews SP, Dore AS, Hollenstein K, Hurrell E, Langmead CJ, Mason JS, Ng IW, Tehan B, Zhukov A, Weir M, Marshall FH J Med Chem. 2012 Mar 8;55(5):1898-903. Epub 2012 Jan 27. PMID:22220592<ref>PMID:22220592</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 3uzc" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_22220592}}, adds the Publication Abstract to the page
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*[[Adenosine A2A receptor 3D structures|Adenosine A2A receptor 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 22220592 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_22220592}}
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__TOC__
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</StructureSection>
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==About this Structure==
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[[3uzc]] 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=3UZC OCA].
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==Reference==
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<ref group="xtra">PMID:022220592</ref><references group="xtra"/>
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Andrews, S P.]]
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[[Category: Large Structures]]
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[[Category: Congreve, M.]]
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[[Category: Andrews SP]]
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[[Category: Dore, A S.]]
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[[Category: Congreve M]]
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[[Category: Hollenstein, K.]]
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[[Category: Dore AS]]
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[[Category: Hurrell, E.]]
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[[Category: Hollenstein K]]
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[[Category: Langmead, C J.]]
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[[Category: Hurrell E]]
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[[Category: Marshall, F H.]]
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[[Category: Langmead CJ]]
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[[Category: Mason, J S.]]
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[[Category: Marshall FH]]
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[[Category: Ng, I W.]]
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[[Category: Mason JS]]
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[[Category: Weir, M.]]
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[[Category: Ng IW]]
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[[Category: Zhukov, A.]]
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[[Category: Weir M]]
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[[Category: 7tm]]
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[[Category: Zhukov A]]
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[[Category: G-protein]]
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[[Category: Gpcr]]
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[[Category: Membrane protein]]
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[[Category: Signaling protein]]
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Current revision

Thermostabilised Adenosine A2A receptor in complex with 4-(3-amino-5-phenyl-1,2,4-triazin-6-yl)-2-chlorophenol

PDB ID 3uzc

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