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==Human Lysophosphatidic Acid Receptor 1-Gi complex bound to ONO-0740556, state4==
<StructureSection load='7yu8' size='340' side='right'caption='[[7yu8]], [[Resolution|resolution]] 5.60&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[7yu8]] is a 5 chain structure with sequence from [https://en.wikipedia.org/wiki/Bos_taurus Bos taurus], [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens], [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus] and [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7YU8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7YU8 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]] 5.6&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=K6L:[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl]+dihydrogen+phosphate'>K6L</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=7yu8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7yu8 OCA], [https://pdbe.org/7yu8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7yu8 RCSB], [https://www.ebi.ac.uk/pdbsum/7yu8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7yu8 ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/GBB1_RAT GBB1_RAT] 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.
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== Publication Abstract from PubMed ==
Lysophosphatidic acid receptor 1 (LPA(1)) is one of the six G protein-coupled receptors activated by the bioactive lipid, lysophosphatidic acid (LPA). LPA(1) is a drug target for various diseases, including cancer, inflammation, and neuropathic pain. Notably, LPA(1) agonists have potential therapeutic value for obesity and urinary incontinence. Here, we report a cryo-electron microscopy structure of the active human LPA(1)-G(i) complex bound to ONO-0740556, an LPA analog with more potent activity against LPA(1). Our structure elucidated the details of the agonist binding mode and receptor activation mechanism mediated by rearrangements of transmembrane segment 7 and the central hydrophobic core. A structural comparison of LPA(1) and other phylogenetically-related lipid-sensing GPCRs identified the structural determinants for lipid preference of LPA(1). Moreover, we characterized the structural polymorphisms at the receptor-G-protein interface, which potentially reflect the G-protein dissociation process. Our study provides insights into the detailed mechanism of LPA(1) binding to agonists and paves the way toward the design of drug-like agonists targeting LPA(1).

Structure of the active G(i)-coupled human lysophosphatidic acid receptor 1 complexed with a potent agonist.,Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O Nat Commun. 2022 Sep 15;13(1):5417. doi: 10.1038/s41467-022-33121-2. PMID:36109516<ref>PMID:36109516</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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<div class="pdbe-citations 7yu8" style="background-color:#fffaf0;"></div>

==See Also==
*[[Lysophosphatidic acid receptor|Lysophosphatidic acid receptor]]
*[[Transducin 3D structures|Transducin 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Bos taurus]]
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Mus musculus]]
[[Category: Rattus norvegicus]]
[[Category: Akasaka H]]
[[Category: Nureki O]]
[[Category: Shihoya W]]