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Regulation of GABAARs by Transmembrane Accessory Proteins
Trends in Neurosciences ( IF 15.9 ) Pub Date : 2021-02-01 , DOI: 10.1016/j.tins.2020.10.011
Wenyan Han 1 , Ryan D Shepard 1 , Wei Lu 1
Affiliation  

The vast majority of fast inhibitory transmission in the brain is mediated by GABA acting on GABAA receptors (GABAARs), which provides inhibitory balance to excitatory drive and controls neuronal output. GABAARs are also effectively targeted by clinically important drugs for treatment in a number of neurological disorders. It has long been hypothesized that function and pharmacology of GABAARs are determined by the channel pore-forming subunits. However, recent studies have provided new dimensions in studying GABAARs due to several transmembrane proteins that interact with GABAARs and modulate their trafficking and function. In this review, we summarize recent findings on these novel GABAAR transmembrane regulators and highlight a potential avenue to develop new GABAAR psychopharmacology by targeting these receptor-associated membrane proteins.

中文翻译:

跨膜辅助蛋白对 GABAAR 的调节

大脑中绝大多数快速抑制传递是由作用于 GABAA 受体 (GABAAR) 的 GABA 介导的,GABAAR 为兴奋性驱动提供抑制平衡并控制神经元输出。GABAAR 也是治疗多种神经系统疾病的临床重要药物的有效靶点。长期以来,人们一直假设 GABAAR 的功能和药理学是由通道成孔亚基决定的。然而,由于多种跨膜蛋白与 GABAAR 相互作用并调节其运输和功能,最近的研究为 GABAAR 的研究提供了新的维度。在这篇综述中,我们总结了这些新型 GABAAR 跨膜调节剂的最新发现,并强调了通过靶向这些受体相关膜蛋白来开发新 GABAAR 精神药理学的潜在途径。
更新日期:2021-02-01
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