6PV8

Human alpha3beta4 nicotinic acetylcholine receptor in complex with AT-1001

6PV8 の概要

• エントリーDOI: 10.2210/pdb6pv8/pdb
• EMDBエントリー: 20488
• 分子名称: Fusion protein of Neuronal acetylcholine receptor subunit alpha-3 and Soluble cytochrome b562, 2-acetamido-2-deoxy-beta-D-glucopyranose, SODIUM ION, ... (12 entities in total)
• 機能のキーワード: ligand-gated ion channel, nicotinic acetylcholine receptor, cys-loop receptor, membrane protein
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 9
• 化学式量合計: 411781.86

構造登録者

Gharpure, A.,Teng, J.,Zhuang, Y.,Noviello, C.M.,Walsh, R.M.,Cabuco, R.,Howard, R.J.,Zaveri, N.T.,Lindahl, E.,Hibbs, R.E. (登録日: 2019-07-19, 公開日: 2019-09-11, 最終更新日: 2024-11-20)

主引用文献

Gharpure, A.,Teng, J.,Zhuang, Y.,Noviello, C.M.,Walsh Jr., R.M.,Cabuco, R.,Howard, R.J.,Zaveri, N.T.,Lindahl, E.,Hibbs, R.E.
Agonist Selectivity and Ion Permeation in the alpha 3 beta 4 Ganglionic Nicotinic Receptor.
Neuron, 104:501-, 2019

PubMed Abstract: Nicotinic acetylcholine receptors are pentameric ion channels that mediate fast chemical neurotransmission. The α3β4 nicotinic receptor subtype forms the principal relay between the central and peripheral nervous systems in the autonomic ganglia. This receptor is also expressed focally in brain areas that affect reward circuits and addiction. Here, we present structures of the α3β4 nicotinic receptor in lipidic and detergent environments, using functional reconstitution to define lipids appropriate for structural analysis. The structures of the receptor in complex with nicotine, as well as the α3β4-selective ligand AT-1001, complemented by molecular dynamics, suggest principles of agonist selectivity. The structures further reveal much of the architecture of the intracellular domain, where mutagenesis experiments and simulations define residues governing ion conductance.

PubMed: 31488329
DOI: 10.1016/j.neuron.2019.07.030

実験手法

ELECTRON MICROSCOPY (3.87 Å)