登録情報 データベース : EMDB / ID : EMD-31500 構造の表示 ダウンロードとリンクタイトル ghrelin-bound ghrelin receptor in complex with Gq マップデータ 詳細 試料複合体 : ghrelin-bound ghrelin receptor in complex with Gqタンパク質・ペプチド : Engineered G-alpha-q subunitタンパク質・ペプチド : Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1タンパク質・ペプチド : Ghrelin-28タンパク質・ペプチド : Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2タンパク質・ペプチド : NB35タンパク質・ペプチド : Soluble cytochrome b562 残り2件を表示 表示を減らすリガンド : OCTANOIC ACID (CAPRYLIC ACID)リガンド : CHOLESTEROL 詳細 キーワード ghrelin / GPCR / Gq / MEMBRANE PROTEIN機能・相同性 機能・相同性情報分子機能 ドメイン・相同性 構成要素
positive regulation of bone development / positive regulation of gastric mucosal blood circulation / ghrelin receptor binding / negative regulation of locomotion / cortisol secretion / growth hormone-releasing hormone activity / negative regulation of circadian sleep/wake cycle, REM sleep / positive regulation of small intestinal transit / regulation of response to food / regulation of gastric motility ... positive regulation of bone development / positive regulation of gastric mucosal blood circulation / ghrelin receptor binding / negative regulation of locomotion / cortisol secretion / growth hormone-releasing hormone activity / negative regulation of circadian sleep/wake cycle, REM sleep / positive regulation of small intestinal transit / regulation of response to food / regulation of gastric motility / regulation of transmission of nerve impulse / positive regulation of circadian sleep/wake cycle, non-REM sleep / positive regulation of cortisol secretion / positive regulation of corticotropin secretion / positive regulation of growth rate / gastric acid secretion / positive regulation of appetite / growth hormone secretion / positive regulation of small intestine smooth muscle contraction / neuronal dense core vesicle lumen / positive regulation of eating behavior / adult feeding behavior / positive regulation of growth hormone secretion / positive regulation of growth hormone receptor signaling pathway / actin polymerization or depolymerization / positive regulation of multicellular organism growth / cartilage development / regulation of postsynapse organization / positive regulation of synapse assembly / positive regulation of vascular endothelial cell proliferation / negative regulation of interleukin-1 beta production / positive regulation of sprouting angiogenesis / negative regulation of endothelial cell proliferation / dendrite development / negative regulation of interleukin-6 production / decidualization / protein tyrosine kinase activator activity / negative regulation of tumor necrosis factor production / response to electrical stimulus / Synthesis, secretion, and deacylation of Ghrelin / positive regulation of insulin secretion involved in cellular response to glucose stimulus / postsynaptic modulation of chemical synaptic transmission / synapse assembly / response to hormone / hormone-mediated signaling pathway / positive regulation of adipose tissue development / negative regulation of angiogenesis / Peptide ligand-binding receptors / excitatory postsynaptic potential / negative regulation of insulin secretion / G protein-coupled receptor binding / positive regulation of insulin secretion / negative regulation of inflammatory response / Schaffer collateral - CA1 synapse / response to estrogen / Olfactory Signaling Pathway / Activation of the phototransduction cascade / G beta:gamma signalling through PLC beta / Presynaptic function of Kainate receptors / Thromboxane signalling through TP receptor / G protein-coupled acetylcholine receptor signaling pathway / glucose metabolic process / G-protein activation / Activation of G protein gated Potassium channels / Inhibition of voltage gated Ca2+ channels via Gbeta/gamma subunits / Prostacyclin signalling through prostacyclin receptor / G beta:gamma signalling through CDC42 / Glucagon signaling in metabolic regulation / G beta:gamma signalling through BTK / Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1) / ADP signalling through P2Y purinoceptor 12 / Sensory perception of sweet, bitter, and umami (glutamate) taste / photoreceptor disc membrane / Glucagon-type ligand receptors / Adrenaline,noradrenaline inhibits insulin secretion / Vasopressin regulates renal water homeostasis via Aquaporins / G alpha (z) signalling events / Glucagon-like Peptide-1 (GLP1) regulates insulin secretion / ADP signalling through P2Y purinoceptor 1 / cellular response to catecholamine stimulus / ADORA2B mediated anti-inflammatory cytokines production / G beta:gamma signalling through PI3Kgamma / Cooperation of PDCL (PhLP1) and TRiC/CCT in G-protein beta folding / adenylate cyclase-activating dopamine receptor signaling pathway / GPER1 signaling / Inactivation, recovery and regulation of the phototransduction cascade / cellular response to prostaglandin E stimulus / G-protein beta-subunit binding / heterotrimeric G-protein complex / G alpha (12/13) signalling events / sensory perception of taste / extracellular vesicle / regulation of cell population proliferation / signaling receptor complex adaptor activity / Thrombin signalling through proteinase activated receptors (PARs) / positive regulation of cold-induced thermogenesis / retina development in camera-type eye / positive regulation of cytosolic calcium ion concentration / GTPase binding / Ca2+ pathway 類似検索 - 分子機能 Preproghrelin peptide / Motilin/ghrelin-associated peptide / Motilin/ghrelin / Motilin/ghrelin-associated peptide / Motilin/ghrelin / G-protein, gamma subunit / G-protein gamma subunit domain profile. / G-protein gamma-like domain / G-protein gamma-like domain superfamily / GGL domain ... Preproghrelin peptide / Motilin/ghrelin-associated peptide / Motilin/ghrelin / Motilin/ghrelin-associated peptide / Motilin/ghrelin / G-protein, gamma subunit / G-protein gamma subunit domain profile. / G-protein gamma-like domain / G-protein gamma-like domain superfamily / GGL domain / G protein gamma subunit-like motifs / GGL domain / G protein beta WD-40 repeat protein / Guanine nucleotide-binding protein, beta subunit / G-protein, beta subunit / G-protein beta WD-40 repeat / WD40 repeat, conserved site / Trp-Asp (WD) repeats signature. / Trp-Asp (WD) repeats profile. / Trp-Asp (WD) repeats circular profile. / WD40 repeats / WD40 repeat / WD40-repeat-containing domain superfamily / WD40/YVTN repeat-like-containing domain superfamily 類似検索 - ドメイン・相同性 Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 / Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 / Appetite-regulating hormone 類似検索 - 構成要素生物種 Homo sapiens (ヒト) / Lama glama (ラマ)手法 単粒子再構成法 / クライオ電子顕微鏡法 / 解像度 : 2.9 Å 詳細 データ登録者Wang Y / Zhuang Y 資金援助 中国, 1件 詳細 詳細を隠すOrganization Grant number 国 National Natural Science Foundation of China (NSFC) 31770796 中国
引用ジャーナル : Nat Commun / 年 : 2021タイトル : Molecular recognition of an acyl-peptide hormone and activation of ghrelin receptor.著者 : Yue Wang / Shimeng Guo / Youwen Zhuang / Ying Yun / Peiyu Xu / Xinheng He / Jia Guo / Wanchao Yin / H Eric Xu / Xin Xie / Yi Jiang / 要旨 : Ghrelin, also called "the hunger hormone", is a gastric peptide hormone that regulates food intake, body weight, as well as taste sensation, reward, cognition, learning and memory. One unique feature ... Ghrelin, also called "the hunger hormone", is a gastric peptide hormone that regulates food intake, body weight, as well as taste sensation, reward, cognition, learning and memory. One unique feature of ghrelin is its acylation, primarily with an octanoic acid, which is essential for its binding and activation of the ghrelin receptor, a G protein-coupled receptor. The multifaceted roles of ghrelin make ghrelin receptor a highly attractive drug target for growth retardation, obesity, and metabolic disorders. Here we present two cryo-electron microscopy structures of G-coupled ghrelin receptor bound to ghrelin and a synthetic agonist, GHRP-6. Analysis of these two structures reveals a unique binding pocket for the octanoyl group, which guides the correct positioning of the peptide to initiate the receptor activation. Together with mutational and functional data, our structures define the rules for recognition of the acylated peptide hormone and activation of ghrelin receptor, and provide structural templates to facilitate drug design targeting ghrelin receptor. 履歴 登録 2021年7月5日 - ヘッダ(付随情報) 公開 2021年8月18日 - マップ公開 2021年8月18日 - 更新 2024年10月30日 - 現状 2024年10月30日 処理サイト : PDBj / 状態 : 公開
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