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	Vestibular modulation by stimulant derivatives in a pentameric ligand-gated ion channel.
ジャーナル・号・ページ	Br J Pharmacol, Vol. 182, Issue 12, Page 2790-2802, Year 2025
掲載日	2025年3月11日
著者	Emelia Karlsson / Olivia Andén / Chen Fan / Zaineb Fourati / Ahmed Haouz / Yuxuan Zhuang / Rebecca J Howard / Marc Delarue / Erik Lindahl /
PubMed 要旨	BACKGROUND AND PURPOSE: Allosteric modulation of pentameric ligand-gated ion channels (pLGICs) are critical for the action of neurotransmitters and many psychoactive drugs. However, details of their ...BACKGROUND AND PURPOSE: Allosteric modulation of pentameric ligand-gated ion channels (pLGICs) are critical for the action of neurotransmitters and many psychoactive drugs. However, details of their modulatory mechanisms remain unclear, especially beyond the orthosteric neurotransmitter-binding sites. The recently reported prokaryotic symbiont of Tevnia jerichonana ligand-gated ion channel (sTeLIC), a pH-gated homologue of eukaryotic receptors in the pLGIC family, is thought to be modulated by aromatic compounds via a relatively uncharacterised modulatory site in the extracellular vestibule. EXPERIMENTAL APPROACH: We have characterised the effects of psychostimulant derivatives on sTeLIC using two-electrode voltage-clamp electrophysiology in the presence and absence of engineered mutations, and determined X-ray and cryo-EM structures of the channel in both closed and open states. KEY RESULTS: We have shown that sTeLIC is sensitive to potentiation by several amphiphilic compounds, which preferentially bind to a vestibular pocket in the contracted open-state extracellular domain. CONCLUSIONS AND IMPLICATIONS: This work provides a detailed structure-function mechanism for allosteric potentiation via a noncanonical ligand site, with potential conservation of the eukaryotic pentameric ligand-gated ion channels.
リンク	Br J Pharmacol / PubMed:40065647
手法	EM (単粒子) / X線回折
解像度	2.19 - 4.16 Å
構造データ	50030 9ex4 EMDB-50030, PDB-9ex4: CryoEM structure of sTeLIC nanodisc in complex with fluorinated fos-choline-8 in open state 手法: EM (単粒子) / 解像度: 2.19 Å 50031 9ex6 EMDB-50031, PDB-9ex6: CryoEM structure of sTeLIC nanodisc in closed state 手法: EM (単粒子) / 解像度: 2.35 Å 50194 9f5n EMDB-50194, PDB-9f5n: CryoEM structure of open sTeLIC in detergent, in complex with n-Dodecyl-Beta-Maltoside 手法: EM (単粒子) / 解像度: 2.56 Å 50195 9f5o EMDB-50195, PDB-9f5o: CryoEM structure of open sTeLIC in detergent, with 4-Bromoamphetamine 手法: EM (単粒子) / 解像度: 4.16 Å PDB-9ewa: The sTeLIC pentameric Ligand-Gated Ion Channel (wild-type) in complex with 4-Bromophenethylamine 手法: X-RAY DIFFRACTION / 解像度: 3.006 Å PDB-9ewl: The sTeLIC pentameric Ligand-Gated Ion Channel (wild-type) in complex with 4-bromoamphetamine 手法: X-RAY DIFFRACTION / 解像度: 3.2 Å
化合物	ChemComp-BNG: nonyl beta-D-glucopyranoside / ノニルβ-D-グルコピラノシド / 可溶化剤YM ChemComp-VMT: 2-(4-bromophenyl)ethanamine / 4-ブロモフェネチルアミン ChemComp-HOH: WATER PDB-1h7r: SCHIFF-BASE COMPLEX OF YEAST 5-AMINOLAEVULINIC ACID DEHYDRATASE WITH SUCCINYLACETONE AT 2.0 A RESOLUTION. PDB-1h8k: A-SPECTRIN SH3 DOMAIN A11V, V23L, M25V, V53I, V58L MUTANT ChemComp-HEX: HEXANE / ヘキサン ChemComp-EPE: 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID / HEPES / pH緩衝剤YM ChemComp-D12: DODECANE / ドデカン ChemComp-OCT: N-OCTANE / オクタン ChemComp-C14: TETRADECANE / テトラデカン ChemComp-D10: DECANE / デカン ChemComp-LMT: DODECYL-BETA-D-MALTOSIDE / ドデシルβ-D-マルトシド / 可溶化剤*YM
由来	endosymbiont of tevnia jerichonana (vent tica) (バクテリア)
キーワード	MEMBRANE PROTEIN / Ion channel / TRANSLOCASE / Pentameric ligand-gated ion channel / cys-loop receptor / pLGIC