2QS1

Crystal structure of the GluR5 ligand binding core dimer in complex with UBP315 at 1.80 Angstroms resolution

2QS1 の概要

• エントリーDOI: 10.2210/pdb2qs1/pdb
• 関連するPDBエントリー: 1TXF 2F34 2F35 2F36 2QS2 2QS3 2QS4
• 分子名称: Glutamate receptor, ionotropic kainate 1, CHLORIDE ION, PENTAETHYLENE GLYCOL, ... (5 entities in total)
• 機能のキーワード: membrane protein, cell junction, glycoprotein, ion transport, ionic channel, phosphorylation, postsynaptic cell membrane, receptor, rna editing, synapse, transmembrane, transport
• 由来する生物種: Rattus norvegicus (rat); 詳細
• 細胞内の位置: Cell membrane; Multi-pass membrane protein: P22756
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 59992.81

構造登録者

Alushin, G.M.,Jane, D.E.,Mayer, M.L. (登録日: 2007-07-30, 公開日: 2008-08-05, 最終更新日: 2023-08-30)

主引用文献

Alushin, G.M.,Jane, D.,Mayer, M.L.
Binding site and ligand flexibility revealed by high resolution crystal structures of GluK1 competitive antagonists.
Neuropharmacology, 60:126-134, 2011

PubMed Abstract: The availability of crystal structures for the ligand binding domains of ionotropic glutamate receptors, combined with their key role in synaptic function in the normal and diseased brain, offers a unique selection of targets for pharmaceutical research compared to other drug targets for which the atomic structure of the ligand binding site is not known. Currently only a few antagonist structures have been solved, and these reveal ligand specific conformational changes that hinder rational drug design. Here we report high resolution crystal structures for three kainate receptor GluK1 antagonist complexes which reveal new and unexpected modes of binding, highlighting the continued need for experimentally determined receptor-ligand complexes.

PubMed: 20558186
DOI: 10.1016/j.neuropharm.2010.06.002

実験手法

X-RAY DIFFRACTION (1.8 Å)