View source for 3vga


==Crystal structure of human adenosine A2A receptor with an allosteric inverse-agonist antibody at 3.1 A resolution==
<StructureSection load='3vga' size='340' side='right'caption='[[3vga]], [[Resolution|resolution]] 3.10&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[3vga]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3VGA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3VGA FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.1&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ZMA:4-{2-[(7-AMINO-2-FURAN-2-YL[1,2,4]TRIAZOLO[1,5-A][1,3,5]TRIAZIN-5-YL)AMINO]ETHYL}PHENOL'>ZMA</scene></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=3vga FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3vga OCA], [https://pdbe.org/3vga PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3vga RCSB], [https://www.ebi.ac.uk/pdbsum/3vga PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3vga ProSAT]</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 ==
G-protein-coupled receptors are the largest class of cell-surface receptors, and these membrane proteins exist in equilibrium between inactive and active states. Conformational changes induced by extracellular ligands binding to G-protein-coupled receptors result in a cellular response through the activation of G proteins. The A(2A) adenosine receptor (A(2A)AR) is responsible for regulating blood flow to the cardiac muscle and is important in the regulation of glutamate and dopamine release in the brain. Here we report the raising of a mouse monoclonal antibody against human A(2A)AR that prevents agonist but not antagonist binding to the extracellular ligand-binding pocket, and describe the structure of A(2A)AR in complex with the antibody Fab fragment (Fab2838). This structure reveals that Fab2838 recognizes the intracellular surface of A(2A)AR and that its complementarity-determining region, CDR-H3, penetrates into the receptor. CDR-H3 is located in a similar position to the G-protein carboxy-terminal fragment in the active opsin structure and to CDR-3 of the nanobody in the active beta(2)-adrenergic receptor structure, but locks A(2A)AR in an inactive conformation. These results suggest a new strategy to modulate the activity of G-protein-coupled receptors.

G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody.,Hino T, Arakawa T, Iwanari H, Yurugi-Kobayashi T, Ikeda-Suno C, Nakada-Nakura Y, Kusano-Arai O, Weyand S, Shimamura T, Nomura N, Cameron AD, Kobayashi T, Hamakubo T, Iwata S, Murata T Nature. 2012 Jan 29;482(7384):237-40. doi: 10.1038/nature10750. PMID:22286059<ref>PMID:22286059</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 3vga" style="background-color:#fffaf0;"></div>

==See Also==
*[[Adenosine A2A receptor 3D structures|Adenosine A2A receptor 3D structures]]
*[[Antibody 3D structures|Antibody 3D structures]]
*[[3D structures of human antibody|3D structures of human antibody]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Mus musculus]]
[[Category: Arakawa T]]
[[Category: Cameron AD]]
[[Category: Hamakubo T]]
[[Category: Hino T]]
[[Category: Ikeda-Suno C]]
[[Category: Iwanari H]]
[[Category: Iwata S]]
[[Category: Kobayashi T]]
[[Category: Kusano-Arai O]]
[[Category: Murata T]]
[[Category: Nakada-Nakura Y]]
[[Category: Nomura N]]
[[Category: Shimamura T]]
[[Category: Weyand S]]
[[Category: Yurugi-Kobayashi T]]