View source for 7p00


==Human Neurokinin 1 receptor (NK1R) substance P Gq chimera (mGsqi) complex==
<StructureSection load='7p00' size='340' side='right'caption='[[7p00]], [[Resolution|resolution]] 2.71&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[7p00]] is a 6 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=7P00 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7P00 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]] 2.71&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=NH2:AMINO+GROUP'>NH2</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=7p00 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7p00 OCA], [https://pdbe.org/7p00 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7p00 RCSB], [https://www.ebi.ac.uk/pdbsum/7p00 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7p00 ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/GBB1_HUMAN GBB1_HUMAN] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction.<ref>PMID:18611381</ref> 
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
The neurokinin 1 receptor (NK(1)R) is involved in inflammation and pain transmission. This pathophysiologically important G protein-coupled receptor is predominantly activated by its cognate agonist substance P (SP) but also by the closely related neurokinins A and B. Here, we report cryo-electron microscopy structures of SP-bound NK(1)R in complex with its primary downstream signal mediators, G(q) and G(s). Our structures reveal how a polar network at the extracellular, solvent-exposed receptor surface shapes the orthosteric pocket and that NK(1)R adopts a noncanonical active-state conformation with an interface for G protein binding, which is distinct from previously reported structures. Detailed comparisons with antagonist-bound NK(1)R crystal structures reveal that insurmountable antagonists induce a distinct and long-lasting receptor conformation that sterically blocks SP binding. Together, our structures provide important structural insights into ligand and G protein promiscuity, the lack of basal signaling, and agonist- and antagonist-induced conformations in the neurokinin receptor family.

Structures of neurokinin 1 receptor in complex with G(q) and G(s) proteins reveal substance P binding mode and unique activation features.,Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A Sci Adv. 2021 Dec 10;7(50):eabk2872. doi: 10.1126/sciadv.abk2872. Epub 2021 Dec , 8. PMID:34878828<ref>PMID:34878828</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 7p00" style="background-color:#fffaf0;"></div>

==See Also==
*[[Transducin 3D structures|Transducin 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Mus musculus]]
[[Category: Ehrenmann J]]
[[Category: Medalia O]]
[[Category: Pluckthun A]]
[[Category: Schoppe J]]
[[Category: Thom C]]
[[Category: Vacca S]]
[[Category: Waltenspuhl Y]]