Stargazin modulates AMPA receptor antagonism

Barbara Cokic

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Stargazin modulates AMPA receptor antagonism

机译：Stargazin调节AMPA受体拮抗作用

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The majority of fast signalling in the brain is mediated by glutamate AMP A (alpha-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate) receptors (AMPARs). AMPARs are associated with auxiliary subunits called transmembrane AMPAR regulatory proteins (TARPs). The first identified member of this family was stargazin. We used two-electrode voltage clamp experiments in Xenopus oocytes to investigate how the association of stargazin to the receptors alters the behaviour of the AMPAR antagonists. We discovered that stargazin decreases the affinity of AMPARs for the competitive antagonist CNQX, which is due to the partial agonistic effect of CNQX in the presence of stargazin. By contrast, stargazin increases the affinity for the non-competitive antagonist GYKI. These findings are important not only for understanding the AMPAR-TARP interaction but also for future therapeutic approaches using AMPAR blockers.

机译：脑中大多数快速信号传导是由谷氨酸AMP A（α-氨基-3-羟基-5-甲基-4-异恶唑-丙酸酯）受体（AMPAR）介导的。 AMPAR与称为跨膜AMPAR调节蛋白（TARP）的辅助亚基相关。该家族的第一个确定成员是stargazin。我们在非洲爪蟾卵母细胞中使用了两电极电压钳实验，以研究stargazin与受体的结合如何改变AMPAR拮抗剂的行为。我们发现，stargazin降低了AMPAR对竞争性拮抗剂CNQX的亲和力，这是由于在stargazin存在时CNQX的部分激动作用。相反，stargazin增加了对非竞争性拮抗剂GYKI的亲和力。这些发现不仅对于理解AMPAR-TARP相互作用非常重要，而且对于使用AMPAR阻滞剂的未来治疗方法也很重要。

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《Futura》 |2010年第1期|p.45-48|共4页
作者
Barbara Cokic;
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作者单位

Synaptic Receptor Trafficking Group, Max Planck Institute of Neurobiology, Martinsried, Germany;

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1. Stargazin modulates AMPA receptor antagonism. [J] . Cokic B, Stein V Neuropharmacology . 2008,第7期

机译：Stargazin调节AMPA受体拮抗作用。
2. AMPA receptors and stargazin-like transmembrane AMPA receptor-regulatory proteins mediate hippocampal kainate neurotoxicity [J] . Susumu Tomita, R. Keith Byrd, Nathalie Rouach, Proceedings of the National Academy of Sciences of the United States of America . 2007,第47期

机译：AMPA受体和stargazin样跨膜AMPA受体调节蛋白介导海马藻酸酯神经毒性
3. Glutamate-Induced AMPA Receptor Desensitization Increases Their Mobility and Modulates Short-Term Plasticity through Unbinding from Stargazin [J] . Constals Audrey, Penn Andrew C., Compans Benjamin, Neuron . 2015,第4期

机译：谷氨酸诱导的AMPA受体脱敏通过从Stargazin解除结合来增加其移动性并调节短期可塑性
4. Optical trapping of quantum-dot conjugated AMPA-type receptors depened on initial assembling states [C] . Tatsunori Kishimoto, Yasuyo Maezawa, Suguru N. Kudoh, SPIE Structured Light Conference . 2018

机译：量子点共轭AMPA型受体的光阱取决于初始组装状态
5. Stargazin and γ-4 Slow the Rate of Channel Opening and Closing of GluA4 AMPA Receptors [D] . Pierce, Vincen. 2018

机译：Stargazin和γ-4减慢了Glua4 AMPA受体的通道打开和关闭速率
6. The Transmembrane AMPA Receptor Regulatory Protein γ4 Is a More Effective Modulator of AMPA Receptor Function than Stargazin (γ2) [O] . Christoph Körber, Markus Werner, Sabine Kott, 2007

机译：跨膜AMPA受体调节蛋白γ4比Stargazin（γ2）更有效地调节AMPA受体功能。
7. The transmembrane AMPA receptor regulatory protein {gamma}4 is a more effective modulator of AMPA receptor function than stargazin ({gamma}2) [O] . Kuf6rber, Christoph, Werner, Markus, Kott, Sabine, 2007

机译：跨膜AMPA受体调节蛋白{gamma} 4是比stargazin（{gamma} 2）更有效的AMPA受体功能调节剂

Stargazin modulates AMPA receptor antagonism

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