7jv5: Difference between revisions

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'''Unreleased structure'''


The entry 7jv5 is ON HOLD
==Cryo-EM structure of SKF-81297-bound dopamine receptor 1 in complex with Gs protein==
<StructureSection load='7jv5' size='340' side='right'caption='[[7jv5]], [[Resolution|resolution]] 3.00&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[7jv5]] is a 5 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7JV5 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7JV5 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&#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=SK0:(1~{R})-6-chloranyl-1-phenyl-2,3,4,5-tetrahydro-1~{H}-3-benzazepine-7,8-diol'>SK0</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=7jv5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7jv5 OCA], [https://pdbe.org/7jv5 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7jv5 RCSB], [https://www.ebi.ac.uk/pdbsum/7jv5 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7jv5 ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/DRD1_HUMAN DRD1_HUMAN] Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
The D1- and D2-dopamine receptors (D1R and D2R), which signal through G(s) and G(i), respectively, represent the principal stimulatory and inhibitory dopamine receptors in the central nervous system. D1R and D2R also represent the main therapeutic targets for Parkinson's disease, schizophrenia, and many other neuropsychiatric disorders, and insight into their signaling is essential for understanding both therapeutic and side effects of dopaminergic drugs. Here, we report four cryoelectron microscopy (cryo-EM) structures of D1R-G(s) and D2R-G(i) signaling complexes with selective and non-selective dopamine agonists, including two currently used anti-Parkinson's disease drugs, apomorphine and bromocriptine. These structures, together with mutagenesis studies, reveal the conserved binding mode of dopamine agonists, the unique pocket topology underlying ligand selectivity, the conformational changes in receptor activation, and potential structural determinants for G protein-coupling selectivity. These results provide both a molecular understanding of dopamine signaling and multiple structural templates for drug design targeting the dopaminergic system.


Authors: Zhang, Y., Xu, P., Mao, C., Wang, L., Krumm, B., Zhou, X.E., Huang, S., Liu, H., Cheng, X., Huang, X.-P., Sheng, D.-D., Xu, T., Liu, Y.-F., Wang, Y., Guo, J., Jiang, Y., Jiang, H., Melcher, K., Roth, B.L., Zhang, Y., Zhang, C., Xu, H.E.
Structural insights into the human D1 and D2 dopamine receptor signaling complexes.,Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE Cell. 2021 Feb 18;184(4):931-942.e18. doi: 10.1016/j.cell.2021.01.027. Epub 2021 , Feb 10. PMID:33571431<ref>PMID:33571431</ref>


Description: Cryo-EM structure of SKF-81297-bound dopamine receptor 1 in complex with Gs protein
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
[[Category: Unreleased Structures]]
</div>
[[Category: Huang, S]]
<div class="pdbe-citations 7jv5" style="background-color:#fffaf0;"></div>
[[Category: Zhou, X.E]]
 
[[Category: Xu, H.E]]
==See Also==
[[Category: Huang, X.-P]]
*[[Dopamine receptor 3D structures|Dopamine receptor 3D structures]]
[[Category: Guo, J]]
*[[Transducin 3D structures|Transducin 3D structures]]
[[Category: Melcher, K]]
== References ==
[[Category: Krumm, B]]
<references/>
[[Category: Jiang, Y]]
__TOC__
[[Category: Wang, Y]]
</StructureSection>
[[Category: Mao, C]]
[[Category: Homo sapiens]]
[[Category: Zhang, Y]]
[[Category: Large Structures]]
[[Category: Sheng, D.-D]]
[[Category: Synthetic construct]]
[[Category: Roth, B.L]]
[[Category: Cheng X]]
[[Category: Xu, P]]
[[Category: Guo J]]
[[Category: Wang, L]]
[[Category: Huang S]]
[[Category: Liu, Y.-F]]
[[Category: Huang X-P]]
[[Category: Jiang, H]]
[[Category: Jiang H]]
[[Category: Cheng, X]]
[[Category: Jiang Y]]
[[Category: Liu, H]]
[[Category: Krumm B]]
[[Category: Zhang, C]]
[[Category: Liu H]]
[[Category: Xu, T]]
[[Category: Liu Y-F]]
[[Category: Mao C]]
[[Category: Melcher K]]
[[Category: Roth BL]]
[[Category: Sheng D-D]]
[[Category: Wang L]]
[[Category: Wang Y]]
[[Category: Xu HE]]
[[Category: Xu P]]
[[Category: Xu T]]
[[Category: Zhang C]]
[[Category: Zhang Y]]
[[Category: Zhou XE]]
[[Category: Zhuang Y]]

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