View source for 8irv


==Dopamine Receptor D5R-Gs-Rotigotine complex==
<StructureSection load='8irv' size='340' side='right'caption='[[8irv]], [[Resolution|resolution]] 3.10&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[8irv]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] 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=8IRV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8IRV 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]] 3.1&#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=PLM:PALMITIC+ACID'>PLM</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>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8irv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8irv OCA], [https://pdbe.org/8irv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8irv RCSB], [https://www.ebi.ac.uk/pdbsum/8irv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8irv ProSAT]</span></td></tr>
</table>
== Disease ==
[https://www.uniprot.org/uniprot/DRD5_HUMAN DRD5_HUMAN] Disease susceptibility may be associated with variants affecting the gene represented in this entry.
== Function ==
[https://www.uniprot.org/uniprot/DRD5_HUMAN DRD5_HUMAN] Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.<ref>PMID:1834671</ref> [https://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX] Electron-transport protein of unknown function.
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== Publication Abstract from PubMed ==
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.

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>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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<div class="pdbe-citations 8irv" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Escherichia coli]]
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Huang S]]
[[Category: Jiang Y]]
[[Category: Li H]]
[[Category: Mao C]]
[[Category: Wang Y]]
[[Category: Xu HE]]
[[Category: Xu P]]
[[Category: Zhang Y]]
[[Category: Zhuang Y]]