8iy6
From Proteopedia
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- | '''Unreleased structure''' | ||
- | + | ==ETB-Gi complex bound to Endotheline-1, focused on receptor== | |
+ | <StructureSection load='8iy6' size='340' side='right'caption='[[8iy6]], [[Resolution|resolution]] 3.13Å' scene=''> | ||
+ | == Structural highlights == | ||
+ | <table><tr><td colspan='2'>[[8iy6]] is a 2 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=8IY6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8IY6 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]] 3.13Å</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=8iy6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8iy6 OCA], [https://pdbe.org/8iy6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8iy6 RCSB], [https://www.ebi.ac.uk/pdbsum/8iy6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8iy6 ProSAT]</span></td></tr> | ||
+ | </table> | ||
+ | <div style="background-color:#fffaf0;"> | ||
+ | == Publication Abstract from PubMed == | ||
+ | The endothelin ET(B) receptor is a promiscuous G-protein coupled receptor that is activated by vasoactive peptide endothelins. ET(B) signaling induces reactive astrocytes in the brain and vasorelaxation in vascular smooth muscle. Consequently, ET(B) agonists are expected to be drugs for neuroprotection and improved anti-tumor drug delivery. Here, we report the cryo-electron microscopy structure of the endothelin-1-ET(B)-G(i) complex at 2.8 A resolution, with complex assembly stabilized by a newly established method. Comparisons with the inactive ET(B) receptor structures revealed how endothelin-1 activates the ET(B) receptor. The NPxxY motif, essential for G-protein activation, is not conserved in ET(B), resulting in a unique structural change upon G-protein activation. Compared with other GPCR-G-protein complexes, ET(B) binds G(i) in the shallowest position, further expanding the diversity of G-protein binding modes. This structural information will facilitate the elucidation of G-protein activation and the rational design of ET(B) agonists. | ||
- | + | Cryo-EM structure of the endothelin-1-ET(B)-G(i) complex.,Sano FK, Akasaka H, Shihoya W, Nureki O Elife. 2023 Apr 25;12:e85821. doi: 10.7554/eLife.85821. PMID:37096326<ref>PMID:37096326</ref> | |
- | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
- | [[Category: | + | </div> |
- | [[Category: | + | <div class="pdbe-citations 8iy6" style="background-color:#fffaf0;"></div> |
- | [[Category: Akasaka | + | == References == |
- | [[Category: Sano | + | <references/> |
- | [[Category: Shihoya | + | __TOC__ |
+ | </StructureSection> | ||
+ | [[Category: Homo sapiens]] | ||
+ | [[Category: Large Structures]] | ||
+ | [[Category: Akasaka H]] | ||
+ | [[Category: Nureki O]] | ||
+ | [[Category: Sano FK]] | ||
+ | [[Category: Shihoya W]] |
Current revision
ETB-Gi complex bound to Endotheline-1, focused on receptor
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