View source for 5unh


==Synchrotron structure of human angiotensin II type 2 receptor in complex with compound 2 (N-[(furan-2-yl)methyl]-N-(4-oxo-2-propyl-3-{[2'-(2H-tetrazol-5-yl)[1,1'- biphenyl]-4-yl]methyl}-3,4-dihydroquinazolin-6-yl)benzamide)==
<StructureSection load='5unh' size='340' side='right'caption='[[5unh]], [[Resolution|resolution]] 2.90&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[5unh]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5UNH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5UNH 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]] 2.9&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=8EM:N-[(FURAN-2-YL)METHYL]-N-(4-OXO-2-PROPYL-3-{[2-(2H-TETRAZOL-5-YL)[1,1-BIPHENYL]-4-YL]METHYL}-3,4-DIHYDROQUINAZOLIN-6-YL)BENZAMIDE'>8EM</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=5unh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5unh OCA], [https://pdbe.org/5unh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5unh RCSB], [https://www.ebi.ac.uk/pdbsum/5unh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5unh ProSAT]</span></td></tr>
</table>
== Disease ==
[https://www.uniprot.org/uniprot/AGTR2_HUMAN AGTR2_HUMAN] X-linked non-syndromic intellectual disability. 
== Function ==
[https://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX] Electron-transport protein of unknown function.[https://www.uniprot.org/uniprot/AGTR2_HUMAN AGTR2_HUMAN] Receptor for angiotensin II. Cooperates with MTUS1 to inhibit ERK2 activation and cell proliferation.<ref>PMID:15123706</ref> 
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
The angiotensin II receptors AT1R and AT2R serve as key components of the renin-angiotensin-aldosterone system. AT1R has a central role in the regulation of blood pressure, but the function of AT2R is unclear and it has a variety of reported effects. To identify the mechanisms that underlie the differences in function and ligand selectivity between these receptors, here we report crystal structures of human AT2R bound to an AT2R-selective ligand and to an AT1R/AT2R dual ligand, capturing the receptor in an active-like conformation. Unexpectedly, helix VIII was found in a non-canonical position, stabilizing the active-like state, but at the same time preventing the recruitment of G proteins or beta-arrestins, in agreement with the lack of signalling responses in standard cellular assays. Structure-activity relationship, docking and mutagenesis studies revealed the crucial interactions for ligand binding and selectivity. Our results thus provide insights into the structural basis of the distinct functions of the angiotensin receptors, and may guide the design of new selective ligands.

Structural basis for selectivity and diversity in angiotensin II receptors.,Zhang H, Han GW, Batyuk A, Ishchenko A, White KL, Patel N, Sadybekov A, Zamlynny B, Rudd MT, Hollenstein K, Tolstikova A, White TA, Hunter MS, Weierstall U, Liu W, Babaoglu K, Moore EL, Katz RD, Shipman JM, Garcia-Calvo M, Sharma S, Sheth P, Soisson SM, Stevens RC, Katritch V, Cherezov V Nature. 2017 Apr 20;544(7650):327-332. doi: 10.1038/nature22035. Epub 2017 Apr 5. PMID:28379944<ref>PMID:28379944</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 5unh" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Escherichia coli]]
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Babaoglu K]]
[[Category: Batyuk A]]
[[Category: Cherezov V]]
[[Category: Garcia-Calvo M]]
[[Category: Han GW]]
[[Category: Hollenstein K]]
[[Category: Hunter MS]]
[[Category: Ishchenko A]]
[[Category: Katritch V]]
[[Category: Katz RD]]
[[Category: Liu W]]
[[Category: Moore EL]]
[[Category: Patel N]]
[[Category: Rudd MT]]
[[Category: Sadybekov A]]
[[Category: Sharma S]]
[[Category: Sheth P]]
[[Category: Shipman JM]]
[[Category: Soisson SM]]
[[Category: Stevens RC]]
[[Category: Tolstikova A]]
[[Category: Weierstall U]]
[[Category: White KL]]
[[Category: White TA]]
[[Category: Zamlynny B]]
[[Category: Zhang H]]