8iru

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m (Protected "8iru" [edit=sysop:move=sysop])
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'''Unreleased structure'''
 
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The entry 8iru is ON HOLD
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==Dopamine Receptor D4R-Gi-Rotigotine complex==
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<StructureSection load='8iru' size='340' side='right'caption='[[8iru]], [[Resolution|resolution]] 3.20&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[8iru]] is a 5 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=8IRU OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8IRU FirstGlance]. <br>
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</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=R5F:(6~{S})-6-[propyl(2-thiophen-2-ylethyl)amino]-5,6,7,8-tetrahydronaphthalen-1-ol'>R5F</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8iru FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8iru OCA], [https://pdbe.org/8iru PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8iru RCSB], [https://www.ebi.ac.uk/pdbsum/8iru PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8iru ProSAT]</span></td></tr>
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</table>
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== Function ==
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[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>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The dopaminergic system, including five dopamine receptors (D1R to D5R), plays essential roles in the central nervous system (CNS); and ligands that activate dopamine receptors have been used to treat many neuropsychiatric disorders, including Parkinson's Disease (PD) and schizophrenia. Here, we report cryo-EM structures of all five subtypes of human dopamine receptors in complex with G protein and bound to the pan-agonist, rotigotine, which is used to treat PD and restless legs syndrome. The structures reveal the basis of rotigotine recognition in different dopamine receptors. Structural analysis together with functional assays illuminate determinants of ligand polypharmacology and selectivity. The structures also uncover the mechanisms of dopamine receptor activation, unique structural features among the five receptor subtypes, and the basis of G protein coupling specificity. Our work provides a comprehensive set of structural templates for the rational design of specific ligands to treat CNS diseases targeting the dopaminergic system.
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Authors: Xu, P., Huang, S., Zhuang, Y., Mao, C., Zhang, Y., Wang, Y., Li, H., Jiang, Y., Zhang, Y., Xu, H.E.
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Structural genomics of the human dopamine receptor system.,Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE Cell Res. 2023 May 23. doi: 10.1038/s41422-023-00808-0. PMID:37221270<ref>PMID:37221270</ref>
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Description: Dopamine Receptor D4R-Gi-Rotigotine complex
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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[[Category: Zhang, Y]]
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<div class="pdbe-citations 8iru" style="background-color:#fffaf0;"></div>
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[[Category: Huang, S]]
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== References ==
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[[Category: Xu, H.E]]
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<references/>
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[[Category: Li, H]]
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__TOC__
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[[Category: Zhuang, Y]]
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</StructureSection>
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[[Category: Xu, P]]
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[[Category: Homo sapiens]]
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[[Category: Jiang, Y]]
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[[Category: Large Structures]]
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[[Category: Wang, Y]]
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[[Category: Mus musculus]]
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[[Category: Mao, C]]
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[[Category: Huang S]]
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[[Category: Jiang Y]]
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[[Category: Li H]]
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[[Category: Mao C]]
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[[Category: Wang Y]]
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[[Category: Xu HE]]
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[[Category: Xu P]]
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[[Category: Zhang Y]]
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[[Category: Zhuang Y]]

Revision as of 09:41, 21 June 2023

Dopamine Receptor D4R-Gi-Rotigotine complex

PDB ID 8iru

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