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	Structural and functional analyses of a GPCR-inhibited ion channel TRPM3.
ジャーナル・号・ページ	Neuron, Vol. 111, Issue 1, Page 81-91.e7, Year 2023
掲載日	2023年1月4日
著者	Chen Zhao / Roderick MacKinnon /
PubMed 要旨	G-protein coupled receptors (GPCRs) govern the physiological response to stimuli by modulating the activity of downstream effectors, including ion channels. TRPM3 is an ion channel inhibited by GPCRs ...G-protein coupled receptors (GPCRs) govern the physiological response to stimuli by modulating the activity of downstream effectors, including ion channels. TRPM3 is an ion channel inhibited by GPCRs through direct interaction with G protein (Gβγ) released upon their activation. This GPCR-TRPM3 signaling pathway contributes to the analgesic effect of morphine. Here, we characterized Gβγ inhibition of TRPM3 using electrophysiology and single particle cryo-electron microscopy (cryo-EM). From electrophysiology, we obtained a half inhibition constant (IC50) of ∼240 nM. Using cryo-EM, we determined structures of mouse TRPM3 expressed in human cells with and without Gβγ and with and without PIP, a lipid required for TRPM3 activity, at resolutions of 2.7-4.7 Å. Gβγ-TRPM3 interfaces vary depending on PIP occupancy; however, in all cases, Gβγ appears loosely attached to TRPM3. The IC50 in electrophysiology experiments raises the possibility that additional unknown factors may stabilize the TRPM3-Gβγ complex.
リンク	Neuron / PubMed:36283409
手法	EM (単粒子)
解像度	2.7 - 4.7 Å
構造データ	27338 8ddq EMDB-27338, PDB-8ddq: cryo-EM structure of TRPM3 ion channel in the presence of soluble Gbg, focused on channel 手法: EM (単粒子) / 解像度: 2.7 Å 27339 8ddr EMDB-27339, PDB-8ddr: cryo-EM structure of TRPM3 ion channel in the absence of PIP2 手法: EM (単粒子) / 解像度: 3.2 Å 27340 8dds EMDB-27340, PDB-8dds: cryo-EM structure of TRPM3 ion channel in the presence of PIP2, state1 手法: EM (単粒子) / 解像度: 3.5 Å 27341 8ddt EMDB-27341, PDB-8ddt: cryo-EM structure of TRPM3 ion channel in the presence of PIP2, state2 手法: EM (単粒子) / 解像度: 3.1 Å 27342 8ddu EMDB-27342, PDB-8ddu: cryo-EM structure of TRPM3 ion channel in the presence of PIP2, state3 手法: EM (単粒子) / 解像度: 3.0 Å 27343 8ddv EMDB-27343, PDB-8ddv: Cryo-EM structure of TRPM3 ion channel in the presence of PIP2, state4 手法: EM (単粒子) / 解像度: 3.2 Å 27344 8ddw EMDB-27344, PDB-8ddw: cryo-EM structure of TRPM3 ion channel in complex with Gbg, tethered by ALFA-nanobody 手法: EM (単粒子) / 解像度: 4.7 Å 27345 8ddx EMDB-27345, PDB-8ddx: cryo-EM structure of TRPM3 ion channel in complex with Gbg in the presence of PIP2, tethered by ALFA-nanobody 手法: EM (単粒子) / 解像度: 3.8 Å 28031 8ed7 EMDB-28031, PDB-8ed7: cryo-EM structure of TRPM3 ion channel in apo state 手法: EM (単粒子) / 解像度: 3.7 Å 28032 8ed8 EMDB-28032, PDB-8ed8: cryo-EM structure of TRPM3 ion channel in the presence of PIP2 and PregS, state 1 手法: EM (単粒子) / 解像度: 3.2 Å 28033 8ed9 EMDB-28033, PDB-8ed9: cryo-EM structure of TRPM3 ion channel in the presence with PIP2 and PregS, state 2 手法: EM (単粒子) / 解像度: 3.4 Å
化合物	ChemComp-3PH: 1,2-DIACYL-GLYCEROL-3-SN-PHOSPHATE / ジステアロイルホスファチジン酸 / ホスファチジン酸 ChemComp-9Z9: (3beta,14beta,17beta,25R)-3-[4-methoxy-3-(methoxymethyl)butoxy]spirost-5-en / 可溶化剤YM ChemComp-NA: Unknown entry / ナトリウムカチオン ChemComp-PIO*: [(2R)-2-octanoyloxy-3-[oxidanyl-[(1R,2R,3S,4R,5R,6S)-2,3,6-tris(oxidanyl)-4,5-diphosphonooxy-cyclohexyl]oxy-phosphoryl]oxy-propyl] octanoate / 1-O-(1-O,2-O-ジオクタノイル-L-グリセロ-3-ホスホ)-D-myo-イノシト-ル4,5-ビスりん酸
由来	mus musculus (ハツカネズミ) homo sapiens (ヒト)
キーワード	MEMBRANE PROTEIN (膜タンパク質) / TRPM3 / ion channel (イオンチャネル) / Gbg / PIP2 (ホスファチジルイノシトール4,5-ビスリン酸)