登録情報 データベース : EMDB / ID : EMD-35815 ダウンロードとリンクタイトル ETB-Gi complex bound to Endotheline-1, focused on receptor マップデータ 詳細 試料複合体 : Complex of Endothelin-1, ETB, and Giタンパク質・ペプチド : Endothelin type B receptorタンパク質・ペプチド : Endothelin-1 詳細 キーワード Class A GPCR / Endothelin / Gi / Vasoactive peptide / PEPTIDE BINDING 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
: / endothelin A receptor binding / rhythmic excitation / negative regulation of phospholipase C/protein kinase C signal transduction / peptide hormone secretion / endothelin B receptor binding / cellular response to human chorionic gonadotropin stimulus / meiotic cell cycle process involved in oocyte maturation / semaphorin-plexin signaling pathway involved in axon guidance / positive regulation of artery morphogenesis ... : / endothelin A receptor binding / rhythmic excitation / negative regulation of phospholipase C/protein kinase C signal transduction / peptide hormone secretion / endothelin B receptor binding / cellular response to human chorionic gonadotropin stimulus / meiotic cell cycle process involved in oocyte maturation / semaphorin-plexin signaling pathway involved in axon guidance / positive regulation of artery morphogenesis / histamine secretion / neural crest cell fate commitment / vein smooth muscle contraction / glomerular endothelium development / response to prostaglandin F / sympathetic neuron axon guidance / positive regulation of sarcomere organization / noradrenergic neuron differentiation / leukocyte activation / phospholipase D-activating G protein-coupled receptor signaling pathway / maternal process involved in parturition / positive regulation of chemokine-mediated signaling pathway / body fluid secretion / rough endoplasmic reticulum lumen / positive regulation of renal sodium excretion / pharyngeal arch artery morphogenesis / regulation of D-glucose transmembrane transport / endothelin receptor signaling pathway involved in heart process / positive regulation of odontogenesis / epithelial fluid transport / cardiac neural crest cell migration involved in outflow tract morphogenesis / negative regulation of hormone secretion / response to ozone / endothelin receptor signaling pathway / Weibel-Palade body / podocyte differentiation / positive regulation of cation channel activity / positive regulation of cell growth involved in cardiac muscle cell development / response to leptin / glomerular filtration / axonogenesis involved in innervation / renal sodium ion absorption / positive regulation of smooth muscle contraction / artery smooth muscle contraction / cellular response to follicle-stimulating hormone stimulus / positive regulation of prostaglandin secretion / respiratory gaseous exchange by respiratory system / vasoconstriction / cellular response to luteinizing hormone stimulus / regulation of pH / cellular response to mineralocorticoid stimulus / basal part of cell / response to salt / positive regulation of urine volume / positive regulation of hormone secretion / regulation of systemic arterial blood pressure by endothelin / cellular response to toxic substance / embryonic heart tube development / dorsal/ventral pattern formation / cellular response to fatty acid / axon extension / cartilage development / positive regulation of neutrophil chemotaxis / prostaglandin biosynthetic process / superoxide anion generation / signal transduction involved in regulation of gene expression / negative regulation of protein metabolic process / middle ear morphogenesis / nitric oxide transport / cellular response to glucocorticoid stimulus / branching involved in blood vessel morphogenesis / positive regulation of cardiac muscle hypertrophy / response to dexamethasone / response to testosterone / negative regulation of smooth muscle cell apoptotic process / thyroid gland development / cAMP/PKA signal transduction / negative regulation of blood coagulation / cellular response to interleukin-1 / membrane depolarization / positive regulation of cell size / canonical Wnt signaling pathway / response to amino acid / regulation of vasoconstriction / cellular response to transforming growth factor beta stimulus / positive regulation of heart rate / transport vesicle / positive regulation of vascular associated smooth muscle cell proliferation / response to muscle stretch / ERK1 and ERK2 cascade / positive regulation of smooth muscle cell proliferation / Transcriptional and post-translational regulation of MITF-M expression and activity / positive regulation of endothelial cell migration / positive regulation of mitotic nuclear division / positive regulation of calcium-mediated signaling / cellular response to calcium ion / Peptide ligand-binding receptors / response to amphetamine / cytokine activity / response to activity 類似検索 - 分子機能 Endothelin-like toxin / Endothelin-like toxin, conserved site / Endothelin / Endothelin family / Endothelin family signature. / Endothelin 類似検索 - ドメイン・相同性生物種 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 : 3.13 Å 詳細 データ登録者Sano FK / Akasaka H / Shihoya W / Nureki O 資金援助 日本, 1件 詳細 詳細を隠すOrganization Grant number 国 Japan Society for the Promotion of Science (JSPS) 21H05037 日本
引用ジャーナル : Elife / 年 : 2023タイトル : Cryo-EM structure of the endothelin-1-ET-G complex.著者 : Fumiya K Sano / Hiroaki Akasaka / Wataru Shihoya / Osamu Nureki / 要旨 : The endothelin ET receptor is a promiscuous G-protein coupled receptor that is activated by vasoactive peptide endothelins. ET signaling induces reactive astrocytes in the brain and vasorelaxation in ... The endothelin ET receptor is a promiscuous G-protein coupled receptor that is activated by vasoactive peptide endothelins. ET signaling induces reactive astrocytes in the brain and vasorelaxation in vascular smooth muscle. Consequently, ET agonists are expected to be drugs for neuroprotection and improved anti-tumor drug delivery. Here, we report the cryo-electron microscopy structure of the endothelin-1-ET-G complex at 2.8 Å resolution, with complex assembly stabilized by a newly established method. Comparisons with the inactive ET receptor structures revealed how endothelin-1 activates the ET receptor. The NPxxY motif, essential for G-protein activation, is not conserved in ET, resulting in a unique structural change upon G-protein activation. Compared with other GPCR-G-protein complexes, ET binds G in the shallowest position, further expanding the diversity of G-protein binding modes. This structural information will facilitate the elucidation of G-protein activation and the rational design of ET agonists. 履歴 登録 2023年4月4日 - ヘッダ(付随情報) 公開 2023年8月16日 - マップ公開 2023年8月16日 - 更新 2025年7月2日 - 現状 2025年7月2日 処理サイト : PDBj / 状態 : 公開
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