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基本情報
登録情報 | ![]() | |||||||||
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タイトル | CryoEM structure of the adenosine 2A receptor-BRIL/Anti BRIL Fab complex with ZM241385 | |||||||||
![]() | Structure of the adenosine 2A receptor-BRIL/Anti BRIL Fab with ZM241385 | |||||||||
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機能・相同性 | ![]() positive regulation of acetylcholine secretion, neurotransmission / positive regulation of circadian sleep/wake cycle, sleep / regulation of norepinephrine secretion / negative regulation of alpha-beta T cell activation / Adenosine P1 receptors / G protein-coupled adenosine receptor activity / G protein-coupled adenosine receptor signaling pathway / response to purine-containing compound / sensory perception / positive regulation of urine volume ...positive regulation of acetylcholine secretion, neurotransmission / positive regulation of circadian sleep/wake cycle, sleep / regulation of norepinephrine secretion / negative regulation of alpha-beta T cell activation / Adenosine P1 receptors / G protein-coupled adenosine receptor activity / G protein-coupled adenosine receptor signaling pathway / response to purine-containing compound / sensory perception / positive regulation of urine volume / NGF-independant TRKA activation / Surfactant metabolism / synaptic transmission, dopaminergic / : / inhibitory postsynaptic potential / negative regulation of vascular permeability / synaptic transmission, cholinergic / type 5 metabotropic glutamate receptor binding / positive regulation of glutamate secretion / blood circulation / response to caffeine / intermediate filament / eating behavior / presynaptic active zone / alpha-actinin binding / membrane depolarization / regulation of calcium ion transport / asymmetric synapse / axolemma / : / cellular defense response / prepulse inhibition / phagocytosis / response to amphetamine / presynaptic modulation of chemical synaptic transmission / excitatory postsynaptic potential / positive regulation of synaptic transmission, glutamatergic / neuron projection morphogenesis / regulation of mitochondrial membrane potential / synaptic transmission, glutamatergic / positive regulation of long-term synaptic potentiation / locomotory behavior / central nervous system development / astrocyte activation / positive regulation of synaptic transmission, GABAergic / positive regulation of protein secretion / apoptotic signaling pathway / electron transport chain / positive regulation of apoptotic signaling pathway / adenylate cyclase-modulating G protein-coupled receptor signaling pathway / adenylate cyclase-activating G protein-coupled receptor signaling pathway / negative regulation of inflammatory response / vasodilation / blood coagulation / cell-cell signaling / presynaptic membrane / G alpha (s) signalling events / postsynaptic membrane / negative regulation of neuron apoptotic process / periplasmic space / electron transfer activity / calmodulin binding / response to xenobiotic stimulus / inflammatory response / iron ion binding / negative regulation of cell population proliferation / neuronal cell body / glutamatergic synapse / lipid binding / apoptotic process / dendrite / heme binding / protein-containing complex binding / regulation of DNA-templated transcription / enzyme binding / identical protein binding / membrane / plasma membrane 類似検索 - 分子機能 | |||||||||
生物種 | ![]() | |||||||||
手法 | 単粒子再構成法 / クライオ電子顕微鏡法 / 解像度: 3.4 Å | |||||||||
![]() | Zhang KH / Wu H / Hoppe N / Manglik A / Cheng YF | |||||||||
資金援助 | ![]()
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![]() | ![]() タイトル: Fusion protein strategies for cryo-EM study of G protein-coupled receptors. 著者: Kaihua Zhang / Hao Wu / Nicholas Hoppe / Aashish Manglik / Yifan Cheng / ![]() 要旨: Single particle cryogenic-electron microscopy (cryo-EM) is used extensively to determine structures of activated G protein-coupled receptors (GPCRs) in complex with G proteins or arrestins. However, ...Single particle cryogenic-electron microscopy (cryo-EM) is used extensively to determine structures of activated G protein-coupled receptors (GPCRs) in complex with G proteins or arrestins. However, applying it to GPCRs without signaling proteins remains challenging because most receptors lack structural features in their soluble domains to facilitate image alignment. In GPCR crystallography, inserting a fusion protein between transmembrane helices 5 and 6 is a highly successful strategy for crystallization. Although a similar strategy has the potential to broadly facilitate cryo-EM structure determination of GPCRs alone without signaling protein, the critical determinants that make this approach successful are not yet clear. Here, we address this shortcoming by exploring different fusion protein designs, which lead to structures of antagonist bound A adenosine receptor at 3.4 Å resolution and unliganded Smoothened at 3.7 Å resolution. The fusion strategies explored here are likely applicable to cryo-EM interrogation of other GPCRs and small integral membrane proteins. #1: ![]() タイトル: Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions 著者: Liu W | |||||||||
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画像 | ![]() | 33.5 KB | ||
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文書・詳細版 | ![]() | 394.5 KB | 表示 | |
XML形式データ | ![]() | 6.3 KB | 表示 | |
CIF形式データ | ![]() | 7.2 KB | 表示 | |
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「今月の分子」の関連する項目 |
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ファイル | ![]() | ||||||||||||||||||||
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注釈 | Structure of the adenosine 2A receptor-BRIL/Anti BRIL Fab with ZM241385 | ||||||||||||||||||||
ボクセルのサイズ | X=Y=Z: 0.835 Å | ||||||||||||||||||||
密度 |
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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 : A2A adenosine receptor-BRIL/Anti BRIL Fab complex
全体 | 名称: A2A adenosine receptor-BRIL/Anti BRIL Fab complex |
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要素 |
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-超分子 #1: A2A adenosine receptor-BRIL/Anti BRIL Fab complex
超分子 | 名称: A2A adenosine receptor-BRIL/Anti BRIL Fab complex / タイプ: complex / キメラ: Yes / ID: 1 / 親要素: 0 / 含まれる分子: #1 |
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由来(天然) | 生物種: ![]() |
組換発現 | 生物種: ![]() |
-分子 #1: Adenosine receptor A2a/Soluble cytochrome b562 Fusion Protein
分子 | 名称: Adenosine receptor A2a/Soluble cytochrome b562 Fusion Protein タイプ: protein_or_peptide / ID: 1 / コピー数: 1 / 光学異性体: LEVO |
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由来(天然) | 生物種: ![]() |
分子量 | 理論値: 43.415855 KDa |
組換発現 | 生物種: ![]() |
配列 | 文字列: VYITVELAIA VLAILGNVLV CWAVWLNSNL QNVTNYFVVS LAAADIAVGV LAIPFAITIS TGFCAACHGC LFIACFVLVL TQSSIFSLL AIAIDRYIAI RIPLRYNGLV TGTRAKGIIA ICWVLSFAIG LTPMLGWNNC GQPKEGKNHS QGCGEGQVAC L FEDVVPMN ...文字列: VYITVELAIA VLAILGNVLV CWAVWLNSNL QNVTNYFVVS LAAADIAVGV LAIPFAITIS TGFCAACHGC LFIACFVLVL TQSSIFSLL AIAIDRYIAI RIPLRYNGLV TGTRAKGIIA ICWVLSFAIG LTPMLGWNNC GQPKEGKNHS QGCGEGQVAC L FEDVVPMN YMVYFNFFAC VLVPLLLMLG VYLRIFLAAR RQLADLEDNW ETLNDNLKVI EKADNAAQVK DALTKMRAAA LD AQKATPP KLEDKSPDSP EMKDFRHGFD ILVGQIDDAL KLANEGKVKE AQAAAEQLKT TRNAYIQKYL ERARSTLQKE VHA AKSLAI IVGLFALCWL PLHIINCFTF FCPDCSHAPL WLMYLAIVLS HTNSVVNPFI YAYRIREFRQ TFRKI |
-分子 #2: 4-{2-[(7-amino-2-furan-2-yl[1,2,4]triazolo[1,5-a][1,3,5]triazin-5...
分子 | 名称: 4-{2-[(7-amino-2-furan-2-yl[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl)amino]ethyl}phenol タイプ: ligand / ID: 2 / コピー数: 1 / 式: ZMA |
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分子量 | 理論値: 337.336 Da |
Chemical component information | ![]() ChemComp-ZMA: |
-実験情報
-構造解析
手法 | クライオ電子顕微鏡法 |
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![]() | 単粒子再構成法 |
試料の集合状態 | cell |
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試料調製
緩衝液 | pH: 7.5 |
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凍結 | 凍結剤: OTHER |
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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: 67.0 e/Å2 |
電子線 | 加速電圧: 300 kV / 電子線源: ![]() |
電子光学系 | 照射モード: SPOT SCAN / 撮影モード: BRIGHT FIELD / 最大 デフォーカス(公称値): 2.0 µm / 最小 デフォーカス(公称値): 1.0 µm |
実験機器 | ![]() モデル: Titan Krios / 画像提供: FEI Company |
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画像解析
最終 再構成 | 解像度のタイプ: BY AUTHOR / 解像度: 3.4 Å / 解像度の算出法: FSC 0.143 CUT-OFF / 使用した粒子像数: 215946 |
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初期 角度割当 | タイプ: ANGULAR RECONSTITUTION |
最終 角度割当 | タイプ: ANGULAR RECONSTITUTION |