4ZZB

The GLIC pentameric Ligand-Gated Ion Channel Locally-closed form complexed to xenon

4ZZB の概要

• エントリーDOI: 10.2210/pdb4zzb/pdb
• 分子名称: Proton-gated ion channel, DODECYL-BETA-D-MALTOSIDE, CHLORIDE ION, ... (6 entities in total)
• 機能のキーワード: membrane protein, transport protein
• 由来する生物種: Gloeobacter violaceus PCC 8105
• タンパク質・核酸の鎖数: 5
• 化学式量合計: 185112.41

構造登録者

Sauguet, L.,Fourati, Z.,Prange, T.,Delarue, M.,Colloc'h, N. (登録日: 2015-05-22, 公開日: 2016-03-02, 最終更新日: 2024-11-13)

主引用文献

Sauguet, L.,Fourati, Z.,Prange, T.,Delarue, M.,Colloc'h, N.
Structural Basis for Xenon Inhibition in a Cationic Pentameric Ligand-Gated Ion Channel.
Plos One, 11:e0149795-e0149795, 2016

PubMed Abstract: GLIC receptor is a bacterial pentameric ligand-gated ion channel whose action is inhibited by xenon. Xenon has been used in clinical practice as a potent gaseous anaesthetic for decades, but the molecular mechanism of interactions with its integral membrane receptor targets remains poorly understood. Here we characterize by X-ray crystallography the xenon-binding sites within both the open and "locally-closed" (inactive) conformations of GLIC. Major binding sites of xenon, which differ between the two conformations, were identified in three distinct regions that all belong to the trans-membrane domain of GLIC: 1) in an intra-subunit cavity, 2) at the interface between adjacent subunits, and 3) in the pore. The pore site is unique to the locally-closed form where the binding of xenon effectively seals the channel. A putative mechanism of the inhibition of GLIC by xenon is proposed, which might be extended to other pentameric cationic ligand-gated ion channels.

PubMed: 26910105
DOI: 10.1371/journal.pone.0149795

実験手法

X-RAY DIFFRACTION (3.4 Å)