登録情報 データベース : PDB / ID : 6o9g 構造の表示 ダウンロードとリンクタイトル Open state GluA2 in complex with STZ and blocked by AgTx-636, after micelle signal subtraction 要素Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit 詳細 キーワード TRANSPORT PROTEIN (運搬体タンパク質) / Ion channel (イオンチャネル)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
LGI-ADAM interactions / eye blink reflex / positive regulation of protein localization to basolateral plasma membrane / Presynaptic depolarization and calcium channel opening / cerebellar mossy fiber / neurotransmitter receptor transport, postsynaptic endosome to lysosome / regulation of AMPA receptor activity / neurotransmitter receptor internalization / channel regulator activity / membrane hyperpolarization ... LGI-ADAM interactions / eye blink reflex / positive regulation of protein localization to basolateral plasma membrane / Presynaptic depolarization and calcium channel opening / cerebellar mossy fiber / neurotransmitter receptor transport, postsynaptic endosome to lysosome / regulation of AMPA receptor activity / neurotransmitter receptor internalization / channel regulator activity / membrane hyperpolarization / Trafficking of AMPA receptors / postsynaptic neurotransmitter receptor diffusion trapping / protein targeting to membrane / neurotransmitter receptor localization to postsynaptic specialization membrane / voltage-gated calcium channel complex / neuromuscular junction development / spine synapse / dendritic spine neck / dendritic spine head / Activation of AMPA receptors / perisynaptic space / transmission of nerve impulse / AMPA glutamate receptor activity / Trafficking of GluR2-containing AMPA receptors / response to lithium ion / 脱分極 / immunoglobulin binding / AMPA glutamate receptor complex / kainate selective glutamate receptor activity / ionotropic glutamate receptor complex / extracellularly glutamate-gated ion channel activity / cellular response to glycine / asymmetric synapse / regulation of receptor recycling / voltage-gated calcium channel activity / Unblocking of NMDA receptors, glutamate binding and activation / glutamate receptor binding / positive regulation of synaptic transmission / presynaptic active zone membrane / glutamate-gated receptor activity / response to fungicide / regulation of synaptic transmission, glutamatergic / somatodendritic compartment / cellular response to brain-derived neurotrophic factor stimulus / dendrite membrane / ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential / ionotropic glutamate receptor binding / cytoskeletal protein binding / ionotropic glutamate receptor signaling pathway / dendrite cytoplasm / hippocampal mossy fiber to CA3 synapse / positive regulation of synaptic transmission, glutamatergic / SNARE binding / dendritic shaft / synaptic membrane / synaptic transmission, glutamatergic / transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential / PDZ domain binding / protein tetramerization / postsynaptic density membrane / Schaffer collateral - CA1 synapse / modulation of chemical synaptic transmission / establishment of protein localization / receptor internalization / terminal bouton / cerebral cortex development / synaptic vesicle membrane / response to calcium ion / endocytic vesicle membrane / シナプス小胞 / presynapse / presynaptic membrane / signaling receptor activity / amyloid-beta binding / 成長円錐 / scaffold protein binding / chemical synaptic transmission / postsynaptic membrane / perikaryon / 樹状突起スパイン / postsynaptic density / neuron projection / 神経繊維 / neuronal cell body / glutamatergic synapse / シナプス / 樹状突起 / protein-containing complex binding / endoplasmic reticulum membrane / protein kinase binding / 細胞膜 / 小胞体 / protein-containing complex / 生体膜 / identical protein binding / 細胞膜 類似検索 - 分子機能 Voltage-dependent calcium channel, gamma-2 subunit / PMP-22/EMP/MP20/Claudin family / Voltage-dependent calcium channel, gamma subunit / PMP-22/EMP/MP20/Claudin superfamily / Bacterial extracellular solute-binding proteins, family 3 / Solute-binding protein family 3/N-terminal domain of MltF / Ionotropic glutamate receptor, metazoa / Ligated ion channel L-glutamate- and glycine-binding site / : / リガンド依存性イオンチャネル ... Voltage-dependent calcium channel, gamma-2 subunit / PMP-22/EMP/MP20/Claudin family / Voltage-dependent calcium channel, gamma subunit / PMP-22/EMP/MP20/Claudin superfamily / Bacterial extracellular solute-binding proteins, family 3 / Solute-binding protein family 3/N-terminal domain of MltF / Ionotropic glutamate receptor, metazoa / Ligated ion channel L-glutamate- and glycine-binding site / : / リガンド依存性イオンチャネル / Ionotropic glutamate receptor, L-glutamate and glycine-binding domain / Ligated ion channel L-glutamate- and glycine-binding site / Ionotropic glutamate receptor / Eukaryotic homologues of bacterial periplasmic substrate binding proteins. / Receptor, ligand binding region / Receptor family ligand binding region / Periplasmic binding protein-like I 類似検索 - ドメイン・相同性 CYCLOTHIAZIDE / グルタミン酸 / Chem-LU7 / GRIA2 / Voltage-dependent calcium channel gamma-2 subunit 類似検索 - 構成要素生物種 Rattus norvegicus (ドブネズミ)Homo sapiens (ヒト)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 : 4.8 Å 詳細データ登録者 Twomey, E.C. / Yelshanskaya, M.V. / Vassilevski, A.A. / Sobolevsky, A.I. 資金援助 米国, 3件 詳細 詳細を隠す組織 認可番号 国 National Institutes of Health/National Institute of Neurological Disorders and Stroke (NIH/NINDS) NS093838 米国 National Institutes of Health/National Institute of Neurological Disorders and Stroke (NIH/NINDS) NS083660 米国 National Institutes of Health/National Cancer Institute (NIH/NCI) CA206573 米国
引用ジャーナル : Neuron / 年 : 2018タイトル : Mechanisms of Channel Block in Calcium-Permeable AMPA Receptors.著者 : Edward C Twomey / Maria V Yelshanskaya / Alexander A Vassilevski / Alexander I Sobolevsky / 要旨 : AMPA receptors mediate fast excitatory neurotransmission and are critical for CNS development and function. Calcium-permeable subsets of AMPA receptors are strongly implicated in acute and chronic ... AMPA receptors mediate fast excitatory neurotransmission and are critical for CNS development and function. Calcium-permeable subsets of AMPA receptors are strongly implicated in acute and chronic neurological disorders. However, despite the clinical importance, the therapeutic landscape for specifically targeting them, and not the calcium-impermeable AMPA receptors, remains largely undeveloped. To address this problem, we used cryo-electron microscopy and electrophysiology to investigate the mechanisms by which small-molecule blockers selectively inhibit ion channel conductance in calcium-permeable AMPA receptors. We determined the structures of calcium-permeable GluA2 AMPA receptor complexes with the auxiliary subunit stargazin bound to channel blockers, including the orb weaver spider toxin AgTx-636, the spider toxin analog NASPM, and the adamantane derivative IEM-1460. Our structures provide insights into the architecture of the blocker binding site and the mechanism of trapping, which are critical for development of small molecules that specifically target calcium-permeable AMPA receptors. 履歴 登録 2019年3月13日 登録サイト : RCSB / 処理サイト : RCSB置き換え 2019年3月20日 ID : 6DM2 改定 1.0 2019年3月20日 Provider : repository / タイプ : Initial release改定 1.1 2019年12月4日 Group : Author supporting evidence / カテゴリ : pdbx_audit_support / Item : _pdbx_audit_support.funding_organization改定 1.2 2019年12月18日 Group : Other / カテゴリ : atom_sitesItem : _atom_sites.fract_transf_matrix[1][1] / _atom_sites.fract_transf_matrix[2][2] / _atom_sites.fract_transf_matrix[3][3]
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