EMDB/PDB/SASBDBから引用されている文献のデータベース

キーワード
構造解析手法	All X線回折 NMR 電子顕微鏡小角散乱中性子線回折線維回折粉末回折赤外分光 EPR FRET 理論モデルハイブリッド
著者・登録者
ジャーナル
IF	>30 >20 >10 >5 all

タイトル	Mechanistic insights into the therapeutic properties of delta opioid receptor.
ジャーナル・号・ページ	Sci Adv, Vol. 12, Issue 13, Page eaeb6737, Year 2026
掲載日	2026年3月27日
著者	Sarah M Bernhard / Susovan Roy Chowdhury / Tsuyoshi Murata / Erin L Reinl / Nokomis Ramos-Gonzalez / Elizabeth Denn / Kevin Appourchaux / Asuka Inoue / Sarah K England / Jonathan F Fay / Susruta Majumdar / Baron Chanda / Tao Che /
PubMed 要旨	The delta opioid receptor (DOR) is a promising target for treating pain, anxiety, and depression, yet no DOR-based drugs have reached the clinic. Here, we examine how ligands with varying therapeutic ...The delta opioid receptor (DOR) is a promising target for treating pain, anxiety, and depression, yet no DOR-based drugs have reached the clinic. Here, we examine how ligands with varying therapeutic properties modulate DOR function. While full agonists rapidly internalize the receptor, partial agonists show a slower rate of internalization, and antagonists increase cell-surface DOR levels. High-resolution structures of ligand-bound DOR-G complexes, including those with antagonists engaged, reveal key interactions that account for DOR ligand selectivity, potency, and efficacy. Single-molecule fluorescence resonance energy transfer studies show that DOR dynamically samples three distinct states (active, obligate preactive, and inactive), and transition rates are tuned by both ligand efficacy and G protein coupling. The endogenous agonist, met-enkephalin, not only stabilizes the active-state conformation but also catalyzes transitions between the active and inactive states. These results reveal how ligand-specific interactions and receptor dynamics can govern pharmacological profiles and provide a framework for developing DOR-targeted therapeutics.
リンク	Sci Adv / PubMed:41880505 / PubMed Central
手法	EM (単粒子)
解像度	3.04 - 3.32 Å
構造データ	71776 9ppw EMDB-71776, PDB-9ppw: CryoEM structure of delta opioid receptor bound to G proteins and Naltrindole 手法: EM (単粒子) / 解像度: 3.32 Å 71777 9ppx EMDB-71777, PDB-9ppx: CryoEM structure of delta opioid receptor bound to G proteins and naltrexone 手法: EM (単粒子) / 解像度: 3.04 Å 71778 9ppy EMDB-71778, PDB-9ppy: CryoEM structure of delta opioid receptor bound to G proteins and met-enkephalin 手法: EM (単粒子) / 解像度: 3.1 Å 71779 9ppz EMDB-71779, PDB-9ppz: CryoEM structure of delta opioid receptor bound to G proteins and SNC80 手法: EM (単粒子) / 解像度: 3.19 Å 71780 9pq0 EMDB-71780, PDB-9pq0: CryoEM structure of delta opioid receptor bound to G proteins and ADL5859 手法: EM (単粒子) / 解像度: 3.12 Å
化合物	ChemComp-EJ4: (4bS,8R,8aS,14bR)-7-(cyclopropylmethyl)-5,6,7,8,14,14b-hexahydro-4,8-methano[1]benzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a(9H)-diol / アンタゴニストYM PDB-1clj: Unknown entry PDB-1cli: X-RAY CRYSTAL STRUCTURE OF AMINOIMIDAZOLE RIBONUCLEOTIDE SYNTHETASE (PURM), FROM THE E. COLI PURINE BIOSYNTHETIC PATHWAY, AT 2.5 A RESOLUTION PDB-1lxy*: Crystal Structure of Arginine Deiminase covalently linked with L-citrulline
由来	homo sapiens (ヒト) mus musculus (ハツカネズミ)
キーワード	MEMBRANE PROTEIN / GPCR / Delta OPIOID Receptor