6-azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) forms an irreversible bond to the active site of the GluR2 AMPA receptor
6-azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) forms an irreversible bond to the active site of the GluR2 AMPA receptor
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DOI：
10.1021/jm701517b
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发表时间：
2008-09-25
影响因子：
7.3
通讯作者：
England, Pamela M.
中科院分区：
文献类型：
--
作者：
Cruz, Leslie A.;Estebanez-Perpina, Eva;England, Pamela M.
AMPA受体介导快速兴奋性突触传递，对突触可塑性至关重要。ANQX是一种光反应性AMPA受体拮抗剂，是一种重要的生物探针，用于不可逆地灭活AMPA受体。在这里，利用x射线晶体学和质谱，我们报告了ANQX在GluR2 AMPAR配体结合核（SIS2J）存在下形成两种主要产物。在光刺激下，ANQX分子内反应生成FQX或分子间反应与Glu705形成共价加合物。
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 (SIS2J). Upon photostimulation, ANQX reacts intramolecularly to form FQX or intermolecularly to form a covalent adduct with Glu705.