View source for 5zkp


==Crystal structure of the human platelet-activating factor receptor in complex with SR 27417==
<StructureSection load='5zkp' size='340' side='right'caption='[[5zkp]], [[Resolution|resolution]] 2.81&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[5zkp]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Desulfovibrio_vulgaris_str._Hildenborough Desulfovibrio vulgaris str. Hildenborough] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5ZKP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5ZKP FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.81&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=9ER:~{N},~{N}-dimethyl-~{N}-(pyridin-3-ylmethyl)-~{N}-[4-[2,4,6-tri(propan-2-yl)phenyl]-1,3-thiazol-2-yl]ethane-1,2-diamine'>9ER</scene>, <scene name='pdbligand=FMN:FLAVIN+MONONUCLEOTIDE'>FMN</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=5zkp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5zkp OCA], [https://pdbe.org/5zkp PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5zkp RCSB], [https://www.ebi.ac.uk/pdbsum/5zkp PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5zkp ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/PTAFR_HUMAN PTAFR_HUMAN] Receptor for platelet activating factor, a chemotactic phospholipid mediator that possesses potent inflammatory, smooth-muscle contractile and hypotensive activity. Seems to mediate its action via a G protein that activates a phosphatidylinositol-calcium second messenger system.<ref>PMID:1281995</ref> <ref>PMID:1374385</ref> <ref>PMID:1656963</ref> <ref>PMID:1657923</ref> [https://www.uniprot.org/uniprot/FLAV_NITV2 FLAV_NITV2] Low-potential electron donor to a number of redox enzymes.
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== Publication Abstract from PubMed ==
Platelet-activating-factor receptor (PAFR) responds to platelet-activating factor (PAF), a phospholipid mediator of cell-to-cell communication that exhibits diverse physiological effects. PAFR is considered an important drug target for treating asthma, inflammation and cardiovascular diseases. Here we report crystal structures of human PAFR in complex with the antagonist SR 27417 and the inverse agonist ABT-491 at 2.8-A and 2.9-A resolution, respectively. The structures, supported by molecular docking of PAF, provide insights into the signal-recognition mechanisms of PAFR. The PAFR-SR 27417 structure reveals an unusual conformation showing that the intracellular tips of helices II and IV shift outward by 13 A and 4 A, respectively, and helix VIII adopts an inward conformation. The PAFR structures, combined with single-molecule FRET and cell-based functional assays, suggest that the conformational change in the helical bundle is ligand dependent and plays a critical role in PAFR activation, thus greatly extending knowledge about signaling by G-protein-coupled receptors.

Structural basis for signal recognition and transduction by platelet-activating-factor receptor.,Cao C, Tan Q, Xu C, He L, Yang L, Zhou Y, Zhou Y, Qiao A, Lu M, Yi C, Han GW, Wang X, Li X, Yang H, Rao Z, Jiang H, Zhao Y, Liu J, Stevens RC, Zhao Q, Zhang XC, Wu B Nat Struct Mol Biol. 2018 Jun;25(6):488-495. doi: 10.1038/s41594-018-0068-y. Epub, 2018 May 28. PMID:29808000<ref>PMID:29808000</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 5zkp" style="background-color:#fffaf0;"></div>
== References ==
<references/>
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</StructureSection>
[[Category: Desulfovibrio vulgaris str. Hildenborough]]
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Cao C]]
[[Category: Wu B]]
[[Category: Zhang XC]]
[[Category: Zhao Q]]