7joz: Difference between revisions
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==Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist== | |||
<StructureSection load='7joz' size='340' side='right'caption='[[7joz]], [[Resolution|resolution]] 3.80Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[7joz]] is a 5 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_virus_T4 Escherichia virus T4], [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Lama_glama Lama glama]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7JOZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7JOZ 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]] 3.8Å</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=VFP:6-(4-furo[3,2-c]pyridin-4-yloxy-2-methyl-phenyl)-1,5-dimethyl-pyrimidine-2,4-dione'>VFP</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=7joz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7joz OCA], [https://pdbe.org/7joz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7joz RCSB], [https://www.ebi.ac.uk/pdbsum/7joz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7joz ProSAT]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Dopamine D1 receptor (D1R) is an important drug target implicated in many psychiatric and neurological disorders. Selective agonism of D1R are sought to be the therapeutic strategy for these disorders. Most selective D1R agonists share a dopamine-like catechol moiety in their molecular structure, and their therapeutic potential is therefore limited by poor pharmacological properties in vivo. Recently, a class of non-catechol D1R selective agonists with a distinct scaffold and pharmacological properties were reported. Here, we report the crystal structure of D1R in complex with stimulatory G protein (Gs) and a non-catechol agonist Compound 1 at 3.8 A resolution. The structure reveals the ligand bound to D1R in an extended conformation, spanning from the orthosteric site to extracellular loop 2 (ECL2). Structural analysis reveals that the unique features of D1R ligand binding pocket explains the remarkable selectivity of this scaffold for D1R over other aminergic receptors, and sheds light on the mechanism for D1R activation by the non-catechol agonist. | |||
Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist.,Sun B, Feng D, Chu ML, Fish I, Lovera S, Sands ZA, Kelm S, Valade A, Wood M, Ceska T, Kobilka TS, Lebon F, Kobilka BK Nat Commun. 2021 Jun 3;12(1):3305. doi: 10.1038/s41467-021-23519-9. PMID:34083522<ref>PMID:34083522</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
[[Category: | <div class="pdbe-citations 7joz" style="background-color:#fffaf0;"></div> | ||
[[Category: | |||
[[Category: Feng | ==See Also== | ||
[[Category: Fish | *[[Dopamine receptor 3D structures|Dopamine receptor 3D structures]] | ||
[[Category: | *[[GTP-binding protein 3D structures|GTP-binding protein 3D structures]] | ||
[[Category: | *[[Transducin 3D structures|Transducin 3D structures]] | ||
[[Category: | == References == | ||
[[Category: | <references/> | ||
[[Category: | __TOC__ | ||
[[Category: | </StructureSection> | ||
[[Category: | [[Category: Escherichia virus T4]] | ||
[[Category: Valade | [[Category: Homo sapiens]] | ||
[[Category: | [[Category: Lama glama]] | ||
[[Category: Large Structures]] | |||
[[Category: Ceska T]] | |||
[[Category: Chu ML]] | |||
[[Category: Feng D]] | |||
[[Category: Fish I]] | |||
[[Category: Kelm S]] | |||
[[Category: Kobilka BK]] | |||
[[Category: Kobilka TS]] | |||
[[Category: Lebon F]] | |||
[[Category: Lovera S]] | |||
[[Category: Sands Z]] | |||
[[Category: Sun B]] | |||
[[Category: Valade A]] | |||
[[Category: Wood M]] | |||
Latest revision as of 08:53, 17 October 2024
Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist
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