7SRQ

5-HT2B receptor bound to LSD obtained by cryo-electron microscopy (cryoEM)

7SRQ の概要

• エントリーDOI: 10.2210/pdb7srq/pdb
• EMDBエントリー: 25401
• 分子名称: 5-hydroxytryptamine receptor 2B, 2-acetamido-2-deoxy-beta-D-glucopyranose, (8alpha)-N,N-diethyl-6-methyl-9,10-didehydroergoline-8-carboxamide (3 entities in total)
• 機能のキーワード: 5-ht2b receptor, serotonin receptor, gpcr, lysergic acid diethylamide, lsd, cryoem, membrane protein
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 35597.27

構造登録者

Barros-Alvarez, X.,Cao, C.,Panova, O.,Roth, B.L.,Skiniotis, G. (登録日: 2021-11-08, 公開日: 2022-09-21, 最終更新日: 2025-05-21)

主引用文献

Cao, C.,Barros-Alvarez, X.,Zhang, S.,Kim, K.,Damgen, M.A.,Panova, O.,Suomivuori, C.M.,Fay, J.F.,Zhong, X.,Krumm, B.E.,Gumpper, R.H.,Seven, A.B.,Robertson, M.J.,Krogan, N.J.,Huttenhain, R.,Nichols, D.E.,Dror, R.O.,Skiniotis, G.,Roth, B.L.
Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD.
Neuron, 110:3154-, 2022

PubMed Abstract: 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 serotonin receptor (HTR2A), the 5-HT 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 β-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.

PubMed: 36087581
DOI: 10.1016/j.neuron.2022.08.006

実験手法

ELECTRON MICROSCOPY (2.7 Å)