7SRR
5-HT2B receptor bound to LSD in complex with heterotrimeric mini-Gq protein obtained by cryo-electron microscopy (cryoEM)
Summary for 7SRR
| Entry DOI | 10.2210/pdb7srr/pdb |
| EMDB information | 25402 |
| Descriptor | G protein subunit q (Gi2-mini-Gq chimera), Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... (6 entities in total) |
| Functional Keywords | 5-ht2b receptor, serotonin receptor, g protein, gpcr, lysergic acid diethylamide, lsd, cryoem, membrane protein |
| Biological source | Homo sapiens More |
| Total number of polymer chains | 5 |
| Total formula weight | 145908.78 |
| Authors | Barros-Alvarez, X.,Kim, K.,Panova, O.,Cao, C.,Roth, B.L.,Skiniotis, G. (deposition date: 2021-11-08, release date: 2022-09-21, Last modification date: 2022-10-19) |
| Primary citation | 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 Cited by 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: 36087581DOI: 10.1016/j.neuron.2022.08.006 PDB entries with the same primary citation |
| Experimental method | ELECTRON MICROSCOPY (2.9 Å) |
Structure validation
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