8F7S

Gi bound delta-opioid receptor in complex with deltorphin

8F7S の概要

• エントリーDOI: 10.2210/pdb8f7s/pdb
• EMDBエントリー: 28907 28908 28909 28911 28912
• 分子名称: Delta-type opioid receptor, deltorphin, Guanine nucleotide-binding protein G(i) subunit alpha-1, ... (7 entities in total)
• 機能のキーワード: delta opioid receptor, g protein coupled receptor, deltorphin, signaling protein
• 由来する生物種: Homo sapiens (human); 詳細
• タンパク質・核酸の鎖数: 8
• 化学式量合計: 219350.68

構造登録者

Wang, Y.,Zhuang, Y.,DiBerto, J.F.,Zhou, X.E.,Schmitz, G.P.,Yuan, Q.,Jain, M.K.,Liu, W.,Melcher, K.,Jiang, Y.,Roth, B.L.,Xu, H.E. (登録日: 2022-11-20, 公開日: 2022-12-14, 最終更新日: 2025-06-04)

主引用文献

Wang, Y.,Zhuang, Y.,DiBerto, J.F.,Zhou, X.E.,Schmitz, G.P.,Yuan, Q.,Jain, M.K.,Liu, W.,Melcher, K.,Jiang, Y.,Roth, B.L.,Xu, H.E.
Structures of the entire human opioid receptor family.
Cell, 186:413-427.e17, 2023

PubMed Abstract: Opioids are effective analgesics, but their use is beset by serious side effects, including addiction and respiratory depression, which contribute to the ongoing opioid crisis. The human opioid system contains four opioid receptors (μOR, δOR, κOR, and NOPR) and a set of related endogenous opioid peptides (EOPs), which show distinct selectivity toward their respective opioid receptors (ORs). Despite being key to the development of safer analgesics, the mechanisms of molecular recognition and selectivity of EOPs to ORs remain unclear. Here, we systematically characterize the binding of EOPs to ORs and present five structures of EOP-OR-G complexes, including β-endorphin- and endomorphin-bound μOR, deltorphin-bound δOR, dynorphin-bound κOR, and nociceptin-bound NOPR. These structures, supported by biochemical results, uncover the specific recognition and selectivity of opioid peptides and the conserved mechanism of opioid receptor activation. These results provide a structural framework to facilitate rational design of safer opioid drugs for pain relief.

PubMed: 36638794
DOI: 10.1016/j.cell.2022.12.026

実験手法

ELECTRON MICROSCOPY (3 Å)