7srr: Difference between revisions
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== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[7srr]] is a 5 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7SRR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7SRR FirstGlance]. <br> | <table><tr><td colspan='2'>[[7srr]] is a 5 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7SRR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7SRR FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=7LD:(8ALPHA)-N,N-DIETHYL-6-METHYL-9,10-DIDEHYDROERGOLINE-8-CARBOXAMIDE'>7LD</scene></td></tr> | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 2.9Å</td></tr> | ||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=7LD:(8ALPHA)-N,N-DIETHYL-6-METHYL-9,10-DIDEHYDROERGOLINE-8-CARBOXAMIDE'>7LD</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=7srr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7srr OCA], [https://pdbe.org/7srr PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7srr RCSB], [https://www.ebi.ac.uk/pdbsum/7srr PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7srr 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=7srr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7srr OCA], [https://pdbe.org/7srr PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7srr RCSB], [https://www.ebi.ac.uk/pdbsum/7srr PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7srr ProSAT]</span></td></tr> | ||
</table> | </table> | ||
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<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
Serotonin (5-hydroxytryptamine [5-HT]) 5-HT2-family receptors represent essential targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the primary psychedelic drug effects are mediated by the 5- | Serotonin (5-hydroxytryptamine [5-HT]) 5-HT2-family receptors represent essential targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the primary psychedelic drug effects are mediated by the 5-HT(2A) serotonin receptor (HTR2A), the 5-HT(2B) serotonin receptor (HTR2B) has been used as a model receptor to study the activation mechanisms of psychedelic drugs due to its high expression and similarity to HTR2A. In this study, we determined the cryo-EM structures of LSD-bound HTR2B in the transducer-free, Gq-protein-coupled, and beta-arrestin-1-coupled states. These structures provide distinct signaling snapshots of LSD's action, ranging from the transducer-free, partially active state to the transducer-coupled, fully active states. Insights from this study will both provide comprehensive molecular insights into the signaling mechanisms of the prototypical psychedelic LSD and accelerate the discovery of novel psychedelic drugs. | ||
Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD.,Cao C, Barros-Alvarez X, Zhang S, Kim K, Damgen MA, Panova O, Suomivuori CM, Fay JF, Zhong X, Krumm BE, Gumpper RH, Seven AB, Robertson MJ, Krogan NJ, Huttenhain R, Nichols DE, Dror RO, Skiniotis G, Roth BL Neuron. 2022 | Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD.,Cao C, Barros-Alvarez X, Zhang S, Kim K, Damgen MA, Panova O, Suomivuori CM, Fay JF, Zhong X, Krumm BE, Gumpper RH, Seven AB, Robertson MJ, Krogan NJ, Huttenhain R, Nichols DE, Dror RO, Skiniotis G, Roth BL Neuron. 2022 Oct 5;110(19):3154-3167.e7. doi: 10.1016/j.neuron.2022.08.006. Epub , 2022 Sep 9. PMID:36087581<ref>PMID:36087581</ref> | ||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
<div class="pdbe-citations 7srr" style="background-color:#fffaf0;"></div> | <div class="pdbe-citations 7srr" style="background-color:#fffaf0;"></div> | ||
==See Also== | |||
*[[Transducin 3D structures|Transducin 3D structures]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
Latest revision as of 09:47, 21 November 2024
5-HT2B receptor bound to LSD in complex with heterotrimeric mini-Gq protein obtained by cryo-electron microscopy (cryoEM)5-HT2B receptor bound to LSD in complex with heterotrimeric mini-Gq protein obtained by cryo-electron microscopy (cryoEM)
Structural highlights
FunctionGBB1_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.[1] Publication Abstract from PubMedSerotonin (5-hydroxytryptamine [5-HT]) 5-HT2-family receptors represent essential targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the primary psychedelic drug effects are mediated by the 5-HT(2A) serotonin receptor (HTR2A), the 5-HT(2B) serotonin receptor (HTR2B) has been used as a model receptor to study the activation mechanisms of psychedelic drugs due to its high expression and similarity to HTR2A. In this study, we determined the cryo-EM structures of LSD-bound HTR2B in the transducer-free, Gq-protein-coupled, and beta-arrestin-1-coupled states. These structures provide distinct signaling snapshots of LSD's action, ranging from the transducer-free, partially active state to the transducer-coupled, fully active states. Insights from this study will both provide comprehensive molecular insights into the signaling mechanisms of the prototypical psychedelic LSD and accelerate the discovery of novel psychedelic drugs. Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD.,Cao C, Barros-Alvarez X, Zhang S, Kim K, Damgen MA, Panova O, Suomivuori CM, Fay JF, Zhong X, Krumm BE, Gumpper RH, Seven AB, Robertson MJ, Krogan NJ, Huttenhain R, Nichols DE, Dror RO, Skiniotis G, Roth BL Neuron. 2022 Oct 5;110(19):3154-3167.e7. doi: 10.1016/j.neuron.2022.08.006. Epub , 2022 Sep 9. PMID:36087581[2] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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