3BKI

Crystal Structure of the GluR2 ligand binding core (S1S2J) in complex with FQX at 1.87 Angstroms

3BKI の概要

• エントリーDOI: 10.2210/pdb3bki/pdb
• 関連するPDBエントリー: 3BKG
• 分子名称: Glutamate receptor 2, [1,2,5]oxadiazolo[3,4-g]quinoxaline-6,7(5H,8H)-dione 1-oxide (3 entities in total)
• 機能のキーワード: ampa receptor, anqx, quinoxaline-2, 3-diones, alternative splicing, cell junction, endoplasmic reticulum, glycoprotein, ion transport, ionic channel, lipoprotein, membrane, palmitate, phosphoprotein, postsynaptic cell membrane, rna editing, synapse, transmembrane, transport, transport protein
• 由来する生物種: Rattus norvegicus (rat); 詳細
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 117767.30

構造登録者

Cruz, L.,Estebanez-Perpina, E.,Pfaff, S.,Borngraeber, S.,Bao, N.,Fletterick, R.,England, P. (登録日: 2007-12-06, 公開日: 2008-09-16, 最終更新日: 2024-10-30)

主引用文献

Cruz, L.A.,Estebanez-Perpina, E.,Pfaff, S.,Borngraeber, S.,Bao, N.,Blethrow, J.,Fletterick, R.J.,England, P.M.
6-Azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) forms an irreversible bond to the active site of the GluR2 AMPA receptor.
J.Med.Chem., 51:5856-5860, 2008

PubMed Abstract: AMPA receptors mediate fast excitatory synaptic transmission and are essential for synaptic plasticity. ANQX, a photoreactive AMPA receptor antagonist, is an important biological probe used to irreversibly inactivate AMPA receptors. Here, using X-ray crystallography and mass spectroscopy, we report that ANQX forms two major products in the presence of the GluR2 AMPAR ligand-binding core (S1S2J). Upon photostimulation, ANQX reacts intramolecularly to form FQX or intermolecularly to form a covalent adduct with Glu705.

PubMed: 18754610
DOI: 10.1021/jm701517b

実験手法

X-RAY DIFFRACTION (1.87 Å)