7wc7: Difference between revisions

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<StructureSection load='7wc7' size='340' side='right'caption='[[7wc7]], [[Resolution|resolution]] 2.60&Aring;' scene=''>
<StructureSection load='7wc7' size='340' side='right'caption='[[7wc7]], [[Resolution|resolution]] 2.60&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[7wc7]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7WC7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7WC7 FirstGlance]. <br>
<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7WC7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7WC7 FirstGlance]. <br>
</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=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=H8G:N,N-diethyl-N-[(8alpha)-6-methyl-9,10-didehydroergolin-8-yl]urea'>H8G</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene></td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.6&#8491;</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=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=H8G:N,N-diethyl-N-[(8alpha)-6-methyl-9,10-didehydroergolin-8-yl]urea'>H8G</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</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=7wc7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7wc7 OCA], [https://pdbe.org/7wc7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7wc7 RCSB], [https://www.ebi.ac.uk/pdbsum/7wc7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7wc7 ProSAT]</span></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=7wc7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7wc7 OCA], [https://pdbe.org/7wc7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7wc7 RCSB], [https://www.ebi.ac.uk/pdbsum/7wc7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7wc7 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
[[https://www.uniprot.org/uniprot/5HT2A_HUMAN 5HT2A_HUMAN]] G-protein coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:1330647, PubMed:18703043, PubMed:19057895). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD) (PubMed:28129538). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors (PubMed:28129538). Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways (PubMed:28129538). Signaling activates phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores (PubMed:18703043, PubMed:28129538). Affects neural activity, perception, cognition and mood (PubMed:18297054). Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction.<ref>PMID:1330647</ref> <ref>PMID:18297054</ref> <ref>PMID:18703043</ref> <ref>PMID:19057895</ref> <ref>PMID:21645528</ref> <ref>PMID:22300836</ref> <ref>PMID:28129538</ref>  (Microbial infection) Acts as a receptor for human JC polyomavirus/JCPyV.<ref>PMID:24089568</ref> 
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Drugs that target the human serotonin 2A receptor (5-HT2AR) are used to treat neuropsychiatric diseases; however, many have hallucinogenic effects, hampering their use. Here, we present structures of 5-HT2AR complexed with the psychedelic drugs psilocin (the active metabolite of psilocybin) and d-lysergic acid diethylamide (LSD), as well as the endogenous neurotransmitter serotonin and the nonhallucinogenic psychedelic analog lisuride. Serotonin and psilocin display a second binding mode in addition to the canonical mode, which enabled the design of the psychedelic IHCH-7113 (a substructure of antipsychotic lumateperone) and several 5-HT2AR beta-arrestin-biased agonists that displayed antidepressant-like activity in mice but without hallucinogenic effects. The 5-HT2AR complex structures presented herein and the resulting insights provide a solid foundation for the structure-based design of safe and effective nonhallucinogenic psychedelic analogs with therapeutic effects.


Structure-based discovery of nonhallucinogenic psychedelic analogs.,Cao D, Yu J, Wang H, Luo Z, Liu X, He L, Qi J, Fan L, Tang L, Chen Z, Li J, Cheng J, Wang S Science. 2022 Jan 28;375(6579):403-411. doi: 10.1126/science.abl8615. Epub 2022, Jan 27. PMID:35084960<ref>PMID:35084960</ref>
==See Also==
 
*[[5-hydroxytryptamine receptor 3D structures|5-hydroxytryptamine receptor 3D structures]]
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 7wc7" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Large Structures]]
[[Category: Large Structures]]
[[Category: Cao, D]]
[[Category: Cao D]]
[[Category: Chen, Z]]
[[Category: Chen Z]]
[[Category: Cheng, J]]
[[Category: Cheng J]]
[[Category: Fan, L]]
[[Category: Fan L]]
[[Category: He, L]]
[[Category: He L]]
[[Category: Li, J]]
[[Category: Li J]]
[[Category: Liu, X]]
[[Category: Liu X]]
[[Category: Luo, Z]]
[[Category: Luo Z]]
[[Category: Qi, J]]
[[Category: Qi J]]
[[Category: Tang, L]]
[[Category: Tang L]]
[[Category: Wang, H]]
[[Category: Wang H]]
[[Category: Wang, S]]
[[Category: Wang S]]
[[Category: Yu, J]]
[[Category: Yu J]]
[[Category: 5-ht]]
[[Category: Lisuride]]
[[Category: Membrane protein]]
[[Category: Serotonin]]
[[Category: Serotonin 2a receptor]]

Latest revision as of 12:18, 17 October 2024

Crystal structure of serotonin 2A receptor in complex with lisurideCrystal structure of serotonin 2A receptor in complex with lisuride

Structural highlights

Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 2.6Å
Ligands:, , , , ,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

See Also

7wc7, resolution 2.60Å

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