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データを開く
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基本情報
| 登録情報 | ![]() | |||||||||
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| タイトル | Structure of GPR55 in complex with G13 and synthetic agonist ML184 | |||||||||
マップデータ | ||||||||||
試料 |
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キーワード | G protein-coupled receptor / GPCR / lipid agonist / cholesterol / MEMBRANE PROTEIN | |||||||||
| 機能・相同性 | 機能・相同性情報D5 dopamine receptor binding / regulation of fibroblast migration / Rho-activating G protein-coupled receptor signaling pathway / cannabinoid receptor activity / negative regulation of adenylate cyclase-activating adrenergic receptor signaling pathway / negative regulation of calcium ion-dependent exocytosis / G protein-coupled adenosine receptor signaling pathway / negative regulation of adenylate cyclase activity / Class A/1 (Rhodopsin-like receptors) / positive regulation of neural precursor cell proliferation ...D5 dopamine receptor binding / regulation of fibroblast migration / Rho-activating G protein-coupled receptor signaling pathway / cannabinoid receptor activity / negative regulation of adenylate cyclase-activating adrenergic receptor signaling pathway / negative regulation of calcium ion-dependent exocytosis / G protein-coupled adenosine receptor signaling pathway / negative regulation of adenylate cyclase activity / Class A/1 (Rhodopsin-like receptors) / positive regulation of neural precursor cell proliferation / negative regulation of synaptic transmission / regulation of small GTPase mediated signal transduction / positive regulation of urine volume / NRAGE signals death through JNK / branching involved in blood vessel morphogenesis / gamma-aminobutyric acid signaling pathway / regulation of calcium ion transport / negative regulation of osteoclast differentiation / positive regulation of Rho protein signal transduction / CDC42 GTPase cycle / negative regulation of apoptotic signaling pathway / regulation of postsynapse assembly / bone resorption / neuronal dense core vesicle / Rho protein signal transduction / positive regulation of vascular associated smooth muscle cell proliferation / positive regulation of superoxide anion generation / RAC1 GTPase cycle / Adenylate cyclase inhibitory pathway / response to nutrient / guanyl-nucleotide exchange factor activity / hippocampal mossy fiber to CA3 synapse / Regulation of insulin secretion / brush border membrane / platelet activation / G protein-coupled receptor binding / G protein-coupled receptor activity / regulation of blood pressure / adenylate cyclase-modulating G protein-coupled receptor signaling pathway / G-protein beta/gamma-subunit complex binding / adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway / Olfactory Signaling Pathway / Activation of the phototransduction cascade / G protein-coupled acetylcholine receptor signaling pathway / G beta:gamma signalling through PLC beta / Presynaptic function of Kainate receptors / Thromboxane signalling through TP receptor / Activation of G protein gated Potassium channels / Inhibition of voltage gated Ca2+ channels via Gbeta/gamma subunits / G-protein activation / Glucagon signaling in metabolic regulation / G beta:gamma signalling through CDC42 / Prostacyclin signalling through prostacyclin receptor / G beta:gamma signalling through BTK / Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1) / photoreceptor disc membrane / ADP signalling through P2Y purinoceptor 12 / melanosome / Sensory perception of sweet, bitter, and umami (glutamate) taste / Glucagon-type ligand receptors / Adrenaline,noradrenaline inhibits insulin secretion / Vasopressin regulates renal water homeostasis via Aquaporins / Glucagon-like Peptide-1 (GLP1) regulates insulin secretion / G alpha (z) signalling events / cellular response to catecholamine stimulus / ADP signalling through P2Y purinoceptor 1 / ADORA2B mediated anti-inflammatory cytokines production / G beta:gamma signalling through PI3Kgamma / adenylate cyclase-activating dopamine receptor signaling pathway / regulation of cell shape / Cooperation of PDCL (PhLP1) and TRiC/CCT in G-protein beta folding / GPER1 signaling / cellular response to prostaglandin E stimulus / heterotrimeric G-protein complex / G-protein beta-subunit binding / G alpha (12/13) signalling events / Inactivation, recovery and regulation of the phototransduction cascade / extracellular vesicle / sensory perception of taste / adenylate cyclase-activating G protein-coupled receptor signaling pathway / Thrombin signalling through proteinase activated receptors (PARs) / signaling receptor complex adaptor activity / retina development in camera-type eye / cell body / GTPase binding / G protein activity / fibroblast proliferation / Ca2+ pathway / midbody / High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells / G alpha (i) signalling events / G alpha (s) signalling events / phospholipase C-activating G protein-coupled receptor signaling pathway / G alpha (q) signalling events / in utero embryonic development / 加水分解酵素; 酸無水物に作用; GTPに作用・細胞または細胞小器官の運動に関与 / Ras protein signal transduction / cell differentiation / positive regulation of ERK1 and ERK2 cascade / cell population proliferation 類似検索 - 分子機能 | |||||||||
| 生物種 | Homo sapiens (ヒト) / ![]() ![]() | |||||||||
| 手法 | 単粒子再構成法 / クライオ電子顕微鏡法 / 解像度: 2.51 Å | |||||||||
データ登録者 | Claff T / Ebenhoch R / Weichert D | |||||||||
| 資金援助 | 1件
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引用 | ジャーナル: Nat Commun / 年: 2025タイトル: Structural basis for lipid-mediated activation of G protein-coupled receptor GPR55. 著者: Tobias Claff / Rebecca Ebenhoch / Jörg T Kley / Aniket Magarkar / Herbert Nar / Dietmar Weichert / ![]() 要旨: GPR55 is an orphan G protein-coupled receptor (GPCR) and represents a promising drug target for cancer, inflammation, and metabolic diseases. The endogenous activation of lipid GPCRs can be solely ...GPR55 is an orphan G protein-coupled receptor (GPCR) and represents a promising drug target for cancer, inflammation, and metabolic diseases. The endogenous activation of lipid GPCRs can be solely mediated by membrane components and different lipids have been proposed as endogenous activators of GPR55, such as cannabinoids and lysophosphatidylinositols. Here, we determine high-resolution cryo-electron microscopy structures of the activated GPR55 in complex with heterotrimeric G and two structurally diverse ligands: the putative endogenous agonist 1-palmitoyl-2-lysophosphatidylinositol (LPI) and the synthetic agonist ML184. These results reveal insights into ligand recognition at GPR55, G protein coupling and receptor activation. Notably, an orthosteric binding site opening towards the membrane is observed in both structures, enabling direct interaction of the agonists with membrane lipids. The structural observations are supported by mutagenesis and functional experiments employing G protein dissociation assays. These findings will be of importance for the structure-based development of drugs targeting GPR55. | |||||||||
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構造の表示
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ダウンロードとリンク
-EMDBアーカイブ
| マップデータ | emd_51284.map.gz | 25.4 MB | EMDBマップデータ形式 | |
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| ヘッダ (付随情報) | emd-51284-v30.xml emd-51284.xml | 25.2 KB 25.2 KB | 表示 表示 | EMDBヘッダ |
| 画像 | emd_51284.png | 65.4 KB | ||
| Filedesc metadata | emd-51284.cif.gz | 7.6 KB | ||
| アーカイブディレクトリ | http://ftp.pdbj.org/pub/emdb/structures/EMD-51284 ftp://ftp.pdbj.org/pub/emdb/structures/EMD-51284 | HTTPS FTP |
-関連構造データ
| 関連構造データ | ![]() 9ge2MC ![]() 9ge3C C: 同じ文献を引用 ( M: このマップから作成された原子モデル |
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| 類似構造データ | 類似検索 - 機能・相同性 F&H 検索 |
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リンク
| EMDBのページ | EMDB (EBI/PDBe) / EMDataResource |
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| 「今月の分子」の関連する項目 |
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マップ
| ファイル | ダウンロード / ファイル: emd_51284.map.gz / 形式: CCP4 / 大きさ: 125 MB / タイプ: IMAGE STORED AS FLOATING POINT NUMBER (4 BYTES) | ||||||||||||||||||||||||||||||||||||
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| 投影像・断面図 | 画像のコントロール
画像は Spider により作成 | ||||||||||||||||||||||||||||||||||||
| ボクセルのサイズ | X=Y=Z: 0.829 Å | ||||||||||||||||||||||||||||||||||||
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| 対称性 | 空間群: 1 | ||||||||||||||||||||||||||||||||||||
| 詳細 | EMDB XML:
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-添付データ
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試料の構成要素
+全体 : Structure of GPR55 in complex with G13 and synthetic agonist ML184
+超分子 #1: Structure of GPR55 in complex with G13 and synthetic agonist ML184
+超分子 #2: Guanine nucleotide-binding proteins
+超分子 #3: Single-chain variable fragment ScFv16
+超分子 #4: G-protein coupled receptor 55 with a GFP tag
+分子 #1: Guanine nucleotide-binding protein G(i) subunit alpha-2,Guanine n...
+分子 #2: Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1
+分子 #3: Single-chain variable fragment ScFv16
+分子 #4: Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
+分子 #5: Green fluorescent protein,G-protein coupled receptor 55,G-protein...
+分子 #7: 3-[4-(2,3-dimethylphenyl)piperazin-1-yl]carbonyl-N,N-dimethyl-4-p...
+分子 #8: CHOLESTEROL
+分子 #9: water
-実験情報
-構造解析
| 手法 | クライオ電子顕微鏡法 |
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解析 | 単粒子再構成法 |
| 試料の集合状態 | particle |
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試料調製
| 緩衝液 | pH: 7.5 |
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| 凍結 | 凍結剤: ETHANE |
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電子顕微鏡法
| 顕微鏡 | FEI TITAN KRIOS |
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| 撮影 | フィルム・検出器のモデル: GATAN K3 (6k x 4k) / 平均電子線量: 45.0 e/Å2 |
| 電子線 | 加速電圧: 300 kV / 電子線源: FIELD EMISSION GUN |
| 電子光学系 | 照射モード: OTHER / 撮影モード: BRIGHT FIELD / 最大 デフォーカス(公称値): 3.0 µm / 最小 デフォーカス(公称値): 0.8 µm / 倍率(公称値): 105000 |
| 実験機器 | ![]() モデル: Titan Krios / 画像提供: FEI Company |
ムービー
コントローラー
万見について




キーワード
Homo sapiens (ヒト)

データ登録者
引用








































X (Sec.)
Y (Row.)
Z (Col.)




















Trichoplusia ni (イラクサキンウワバ)

解析
FIELD EMISSION GUN
