View source for 5ung


==XFEL structure of human angiotensin II type 2 receptor (Orthorhombic form) in complex with compound 1 (N-benzyl-N-(2-ethyl-4-oxo-3-{[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl] methyl}-3,4-dihydroquinazolin-6-yl)thiophene-2-carboxamide)==
<StructureSection load='5ung' size='340' side='right' caption='[[5ung]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[5ung]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5UNG OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5UNG FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=8ES:N-BENZYL-N-(2-ETHYL-4-OXO-3-{[2-(2H-TETRAZOL-5-YL)[1,1-BIPHENYL]-4-YL]METHYL}-3,4-DIHYDROQUINAZOLIN-6-YL)THIOPHENE-2-CARBOXAMIDE'>8ES</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene></td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5unf|5unf]], [[5unh|5unh]]</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=5ung FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ung OCA], [http://pdbe.org/5ung PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5ung RCSB], [http://www.ebi.ac.uk/pdbsum/5ung PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5ung ProSAT]</span></td></tr>
</table>
== Function ==
[[http://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX]] Electron-transport protein of unknown function. 
<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 5ung" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Babaoglu, K]]
[[Category: Batyuk, A]]
[[Category: Cherezov, V]]
[[Category: Garcia-Calvo, M]]
[[Category: Han, G W]]
[[Category: Hollenstein, K]]
[[Category: Hunter, M S]]
[[Category: Ishchenko, A]]
[[Category: Katritch, V]]
[[Category: Katz, R D]]
[[Category: Liu, W]]
[[Category: Moore, E L]]
[[Category: Patel, N]]
[[Category: Rudd, M T]]
[[Category: Sadybekov, A]]
[[Category: Sharma, S]]
[[Category: Sheth, P]]
[[Category: Shipman, J M]]
[[Category: Soisson, S M]]
[[Category: Stevens, R C]]
[[Category: Tolstikova, A]]
[[Category: Weierstall, U]]
[[Category: White, K L]]
[[Category: White, T A]]
[[Category: Zamlynny, B]]
[[Category: Zhang, H]]
[[Category: Blood pressure regulation]]
[[Category: Bril]]
[[Category: Gpcr]]
[[Category: Gpcr signaling]]
[[Category: Human angiotensin ii receptor complex]]
[[Category: Lcp]]
[[Category: Membrane protein]]
[[Category: Orthorhombic crystal]]
[[Category: Signaling protein]]
[[Category: Xfel]]