EMDB/PDB/SASBDBから引用されている文献のデータベース

キーワード
構造解析手法	All X線回折 NMR 電子顕微鏡小角散乱中性子線回折線維回折粉末回折赤外分光 EPR FRET 理論モデルハイブリッド
著者・登録者
ジャーナル
IF	>30 >20 >10 >5 all

タイトル	Mechanism of NMDA Receptor Inhibition and Activation.
ジャーナル・号・ページ	Cell, Vol. 165, Issue 3, Page 704-714, Year 2016
掲載日	2016年4月21日
著者	Shujia Zhu / Richard A Stein / Craig Yoshioka / Chia-Hsueh Lee / April Goehring / Hassane S Mchaourab / Eric Gouaux /
PubMed 要旨	N-methyl-D-aspartate receptors (NMDARs) are glutamate-gated, calcium-permeable ion channels that mediate synaptic transmission and underpin learning and memory. NMDAR dysfunction is directly ...N-methyl-D-aspartate receptors (NMDARs) are glutamate-gated, calcium-permeable ion channels that mediate synaptic transmission and underpin learning and memory. NMDAR dysfunction is directly implicated in diseases ranging from seizure to ischemia. Despite its fundamental importance, little is known about how the NMDAR transitions between inactive and active states and how small molecules inhibit or activate ion channel gating. Here, we report electron cryo-microscopy structures of the GluN1-GluN2B NMDA receptor in an ensemble of competitive antagonist-bound states, an agonist-bound form, and a state bound with agonists and the allosteric inhibitor Ro25-6981. Together with double electron-electron resonance experiments, we show how competitive antagonists rupture the ligand binding domain (LBD) gating "ring," how agonists retain the ring in a dimer-of-dimers configuration, and how allosteric inhibitors, acting within the amino terminal domain, further stabilize the LBD layer. These studies illuminate how the LBD gating ring is fundamental to signal transduction and gating in NMDARs.
リンク	Cell / PubMed:27062927 / PubMed Central
手法	EM (単粒子)
解像度	7.0 - 15.4 Å
構造データ	8097 5iou EMDB-8097, PDB-5iou: Cryo-EM structure of GluN1/GluN2B NMDA receptor in the glutamate/glycine-bound conformation 手法: EM (単粒子) / 解像度: 7.0 Å 8098 5iov EMDB-8098, PDB-5iov: Cryo-EM structure of GluN1/GluN2B NMDA receptor in the glutamate/glycine/Ro25-6981-bound conformation 手法: EM (単粒子) / 解像度: 7.5 Å 8101 5ipq EMDB-8101, PDB-5ipq: Cryo-EM structure of GluN1/GluN2B NMDA receptor in the DCKA/D-APV-bound conformation, state 2 手法: EM (単粒子) / 解像度: 13.5 Å 8102 5ipr EMDB-8102, PDB-5ipr: Cryo-EM structure of GluN1/GluN2B NMDA receptor in the DCKA/D-APV-bound conformation, state 3 手法: EM (単粒子) / 解像度: 14.1 Å 8103 5ips EMDB-8103, PDB-5ips: Cryo-EM structure of GluN1/GluN2B NMDA receptor in the DCKA/D-APV-bound conformation, state 4 手法: EM (単粒子) / 解像度: 13.5 Å 8104 5ipt EMDB-8104, PDB-5ipt: Cryo-EM structure of GluN1/GluN2B NMDA receptor in the DCKA/D-APV-bound conformation, state 5 手法: EM (単粒子) / 解像度: 14.1 Å 8105 5ipu EMDB-8105, PDB-5ipu: Cryo-EM structure of GluN1/GluN2B NMDA receptor in the DCKA/D-APV-bound conformation, state 6 手法: EM (単粒子) / 解像度: 15.4 Å 8106 5ipv EMDB-8106, PDB-5ipv: Cryo-EM structure of GluN1/GluN2B NMDA receptor in the DCKA/D-APV-bound conformation, state 1 手法: EM (単粒子) / 解像度: 9.25 Å
化合物	ChemComp-GLY: GLYCINE / グリシン / グリシン ChemComp-GLU: GLUTAMIC ACID / グルタミン酸 / グルタミン酸 ChemComp-QEM: 4-[(1R,2S)-3-(4-benzylpiperidin-1-yl)-1-hydroxy-2-methylpropyl]phenol / Ro-25-6981
由来	xenopus laevis (アフリカツメガエル)
キーワード	SIGNALING PROTEIN / ligand-gated ion channel (リガンド依存性イオンチャネル) / synaptic transmission