View source for 7ymh


==Cryo-EM structure of Nb29-alpha1AAR-miniGsq complex bound to noradrenaline==
<StructureSection load='7ymh' size='340' side='right'caption='[[7ymh]], [[Resolution|resolution]] 3.52&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[7ymh]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7YMH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7YMH FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 3.52&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=E5E:[(2~{R})-2-[3,4-bis(oxidanyl)phenyl]-2-oxidanyl-ethyl]azanium'>E5E</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=7ymh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7ymh OCA], [https://pdbe.org/7ymh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7ymh RCSB], [https://www.ebi.ac.uk/pdbsum/7ymh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7ymh ProSAT]</span></td></tr>
</table>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
The alpha(1A-)adrenergic receptor (alpha(1A)AR) belongs to the family of G protein-coupled receptors that respond to adrenaline and noradrenaline. alpha(1A)AR is involved in smooth muscle contraction and cognitive function. Here, we present three cryo-electron microscopy structures of human alpha(1A)AR bound to the endogenous agonist noradrenaline, its selective agonist oxymetazoline, and the antagonist tamsulosin, with resolutions range from 2.9 A to 3.5 A. Our active and inactive alpha(1A)AR structures reveal the activation mechanism and distinct ligand binding modes for noradrenaline compared with other adrenergic receptor subtypes. In addition, we identified a nanobody that preferentially binds to the extracellular vestibule of alpha(1A)AR when bound to the selective agonist oxymetazoline. These results should facilitate the design of more selective therapeutic drugs targeting both orthosteric and allosteric sites in this receptor family.

Structural basis of alpha(1A)-adrenergic receptor activation and recognition by an extracellular nanobody.,Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X Nat Commun. 2023 Jun 20;14(1):3655. doi: 10.1038/s41467-023-39310-x. PMID:37339967<ref>PMID:37339967</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 7ymh" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Synthetic construct]]
[[Category: Kobilka BK]]
[[Category: Liu X]]
[[Category: Toyoda Y]]
[[Category: Yan C]]
[[Category: Zhu A]]