التفاصيل البيبلوغرافية
| العنوان: |
Structure of the µ-opioid receptor–Gi protein complex |
| المؤلفون: |
Koehl, Antoine, Hu, Hongli, Maeda, Shoji, Zhang, Yan, Qu, Qianhui, Paggi, Joseph M, Latorraca, Naomi R, Hilger, Daniel, Dawson, Roger, Matile, Hugues, Schertler, Gebhard FX, Granier, Sebastien, Weis, William I, Dror, Ron O, Manglik, Aashish, Skiniotis, Georgios, Kobilka, Brian K |
| المصدر: |
Nature, vol 558, iss 7711 |
| بيانات النشر: |
eScholarship, University of California |
| سنة النشر: |
2018 |
| المجموعة: |
University of California: eScholarship |
| مصطلحات موضوعية: |
Drug Abuse (NIDA only), Pain Research, Substance Misuse, Generic health relevance, Animals, Binding Sites, Cryoelectron Microscopy, Enkephalin, Ala(2)-MePhe(4)-Gly(5)-, Female, GTP-Binding Protein alpha Subunits, Gi-Go, Gs, Humans, Ligands, Mice, Inbred BALB C, Molecular Dynamics Simulation, Morphinans, Protein Stability, Receptors, Adrenergic, beta-2, Opioid, mu, Substrate Specificity, General Science & Technology |
| جغرافية الموضوع: |
547 - 552 |
| الوصف: |
The μ-opioid receptor (μOR) is a G-protein-coupled receptor (GPCR) and the target of most clinically and recreationally used opioids. The induced positive effects of analgesia and euphoria are mediated by μOR signalling through the adenylyl cyclase-inhibiting heterotrimeric G protein Gi. Here we present the 3.5 Å resolution cryo-electron microscopy structure of the μOR bound to the agonist peptide DAMGO and nucleotide-free Gi. DAMGO occupies the morphinan ligand pocket, with its Nterminus interacting with conserved receptor residues and its Cterminus engaging regions important for opioid-ligand selectivity. Comparison of the μOR-Gi complex to previously determined structures of other GPCRs bound to the stimulatory G protein Gs reveals differences in the position of transmembrane receptor helix 6 and in the interactions between the G protein α-subunit and the receptor core. Together, these results shed light on the structural features that contribute to the Gi protein-coupling specificity of the µOR. |
| نوع الوثيقة: |
article in journal/newspaper |
| وصف الملف: |
application/pdf |
| اللغة: |
unknown |
| العلاقة: |
qt1rb3n024; https://escholarship.org/uc/item/1rb3n024Test |
| الإتاحة: |
https://escholarship.org/uc/item/1rb3n024Test |
| حقوق: |
public |
| رقم الانضمام: |
edsbas.808D5D61 |
| قاعدة البيانات: |
BASE |
