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基本情報
登録情報 | データベース: PDB / ID: 8iy6 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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タイトル | ETB-Gi complex bound to Endotheline-1, focused on receptor | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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![]() | PEPTIDE BINDING PROTEIN / Class A GPCR / Endothelin / Gi / Vasoactive peptide | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
機能・相同性 | ![]() : / 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 / Weibel-Palade body / endothelin receptor signaling pathway / podocyte differentiation / positive regulation of cation channel activity / positive regulation of cell growth involved in cardiac muscle cell development / response to leptin / axonogenesis involved in innervation / glomerular filtration / renal sodium ion absorption / positive regulation of smooth muscle contraction / artery smooth muscle contraction / positive regulation of prostaglandin secretion / cellular response to follicle-stimulating hormone stimulus / cellular response to luteinizing hormone stimulus / vasoconstriction / respiratory gaseous exchange by respiratory system / regulation of pH / cellular response to mineralocorticoid stimulus / basal part of cell / response to salt / positive regulation of urine volume / regulation of systemic arterial blood pressure by endothelin / positive regulation of hormone secretion / cellular response to toxic substance / dorsal/ventral pattern formation / embryonic heart tube development / cellular response to fatty acid / cartilage development / axon extension / 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 / response to dexamethasone / positive regulation of cardiac muscle hypertrophy / response to testosterone / negative regulation of smooth muscle cell apoptotic process / thyroid gland development / cAMP/PKA signal transduction / membrane depolarization / cellular response to interleukin-1 / negative regulation of blood coagulation / 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 / response to activity / cytokine activity 類似検索 - 分子機能 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
生物種 | ![]() | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
手法 | 電子顕微鏡法 / 単粒子再構成法 / クライオ電子顕微鏡法 / 解像度: 3.13 Å | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
![]() | Sano, F.K. / Akasaka, H. / Shihoya, W. / Nureki, O. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
資金援助 | ![]()
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![]() | ![]() 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 |
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構造の表示
構造ビューア | 分子: ![]() ![]() |
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ダウンロードとリンク
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ダウンロード
PDBx/mmCIF形式 | ![]() | 93.9 KB | 表示 | ![]() |
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PDB形式 | ![]() | 61.2 KB | 表示 | ![]() |
PDBx/mmJSON形式 | ![]() | ツリー表示 | ![]() | |
その他 | ![]() |
-検証レポート
文書・要旨 | ![]() | 992 KB | 表示 | ![]() |
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文書・詳細版 | ![]() | 994.2 KB | 表示 | |
XML形式データ | ![]() | 14.3 KB | 表示 | |
CIF形式データ | ![]() | 20 KB | 表示 | |
アーカイブディレクトリ | ![]() ![]() | HTTPS FTP |
-関連構造データ
関連構造データ | ![]() 35815MC ![]() 8iy5C M: このデータのモデリングに利用したマップデータ C: 同じ文献を引用 ( |
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類似構造データ | 類似検索 - 機能・相同性 ![]() |
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リンク
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集合体
登録構造単位 | ![]()
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1 |
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要素
#1: タンパク質 | 分子量: 67492.219 Da / 分子数: 1 / 由来タイプ: 組換発現 / 由来: (組換発現) ![]() 発現宿主: ![]() ![]() 株 (発現宿主): Sf9 cells |
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#2: タンパク質・ペプチド | 分子量: 2497.951 Da / 分子数: 1 / 由来タイプ: 合成 / 由来: (合成) ![]() |
Has protein modification | Y |
-実験情報
-実験
実験 | 手法: 電子顕微鏡法 |
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EM実験 | 試料の集合状態: PARTICLE / 3次元再構成法: 単粒子再構成法 |
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試料調製
構成要素 | 名称: Complex of Endothelin-1, ETB, and Gi / タイプ: COMPLEX / Entity ID: all / 由来: RECOMBINANT |
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由来(天然) | 生物種: ![]() |
由来(組換発現) | 生物種: ![]() ![]() |
緩衝液 | pH: 8 |
試料 | 濃度: 8 mg/ml / 包埋: NO / シャドウイング: NO / 染色: NO / 凍結: YES |
試料支持 | グリッドの材料: GOLD / グリッドのサイズ: 300 divisions/in. / グリッドのタイプ: Quantifoil R1.2/1.3 |
急速凍結 | 凍結剤: ETHANE |
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電子顕微鏡撮影
実験機器 | ![]() モデル: Titan Krios / 画像提供: FEI Company |
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顕微鏡 | モデル: FEI TITAN KRIOS |
電子銃 | 電子線源: ![]() |
電子レンズ | モード: BRIGHT FIELD / 倍率(公称値): 105000 X / 最大 デフォーカス(公称値): 1600 nm / 最小 デフォーカス(公称値): 800 nm / Cs: 2.7 mm |
試料ホルダ | 凍結剤: NITROGEN |
撮影 | 平均露光時間: 2.3 sec. / 電子線照射量: 50 e/Å2 / フィルム・検出器のモデル: GATAN K3 (6k x 4k) / 実像数: 10408 |
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解析
EMソフトウェア | 名称: PHENIX / カテゴリ: モデル精密化 | ||||||||||||||||||||||||
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CTF補正 | タイプ: PHASE FLIPPING AND AMPLITUDE CORRECTION | ||||||||||||||||||||||||
3次元再構成 | 解像度: 3.13 Å / 解像度の算出法: FSC 0.143 CUT-OFF / 粒子像の数: 260085 / 対称性のタイプ: POINT | ||||||||||||||||||||||||
精密化 | 解像度: 3.13→3.13 Å / Cor.coef. Fo:Fc: 0.877 / SU B: 20.883 / SU ML: 0.372 / ESU R: 0.39 立体化学のターゲット値: MAXIMUM LIKELIHOOD WITH PHASES 詳細: HYDROGENS HAVE BEEN ADDED IN THE RIDING POSITIONS
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溶媒の処理 | 溶媒モデル: PARAMETERS FOR MASK CACLULATION | ||||||||||||||||||||||||
原子変位パラメータ | Biso mean: 84.927 Å2 | ||||||||||||||||||||||||
精密化ステップ | サイクル: 1 / 合計: 2495 | ||||||||||||||||||||||||
拘束条件 |
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LS精密化 シェル | 解像度: 3→3.078 Å / Total num. of bins used: 20 /
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