4U4G

Structure of GluA2* in complex with competitive antagonist ZK 200775

4U4G の概要

• エントリーDOI: 10.2210/pdb4u4g/pdb
• 関連するPDBエントリー: 4U4F
• 分子名称: Glutamate receptor 2, beta-D-mannopyranose-(1-3)-beta-D-mannopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid (3 entities in total)
• 機能のキーワード: ionotropic glutamate receptor, ampa receptor, competitive antagonist, tetramer, complex, transport protein
• 由来する生物種: Rattus norvegicus (Rat)
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 373585.02

構造登録者

Yelshanskaya, M.V.,Li, M.,Sobolevsky, A.I. (登録日: 2014-07-23, 公開日: 2014-10-22, 最終更新日: 2024-11-06)

主引用文献

Yelshanskaya, M.V.,Li, M.,Sobolevsky, A.I.
Structure of an agonist-bound ionotropic glutamate receptor.
Science, 345:1070-1074, 2014

PubMed Abstract: Ionotropic glutamate receptors (iGluRs) mediate most excitatory neurotransmission in the central nervous system and function by opening their ion channel in response to binding of agonist glutamate. Here, we report a structure of a homotetrameric rat GluA2 receptor in complex with partial agonist (S)-5-nitrowillardiine. Comparison of this structure with the closed-state structure in complex with competitive antagonist ZK 200775 suggests conformational changes that occur during iGluR gating. Guided by the structures, we engineered disulfide cross-links to probe domain interactions that are important for iGluR gating events. The combination of structural information, kinetic modeling, and biochemical and electrophysiological experiments provides insight into the mechanism of iGluR gating.

PubMed: 25103407
DOI: 10.1126/science.1256508

実験手法

X-RAY DIFFRACTION (4.49 Å)