Mayer Mark L
Laboratory of Cellular and Molecular Neurophysiology, Porter Neuroscience Research Center, Building 35 Room 3B 1002 MSC 3712, 35 Lincoln Drive, Bethesda, MD 20892-3712, USA.
Curr Opin Neurobiol. 2005 Jun;15(3):282-8. doi: 10.1016/j.conb.2005.05.004.
Glutamate receptor ion channels mediate excitatory responses at the majority of CNS synapses. They are the only ligand-gated ion channels for which multiple high-resolution crystal structures have been solved. Highlights of information gained from mechanistic studies based on the crystal structures of their ligand-binding domains include explanations for strikingly diverse phenomena. These include the basis for subtype-specific agonist selectivity; mechanisms for desensitization and allosteric modulation; and mechanisms for partial agonist activity. In addition, multiple lines of evidence, including low-resolution electron microscopic studies, suggest that native AMPA receptors combine with an auxiliary subunit which regulates activity and trafficking. Functional studies suggest that glutamate receptor gating is distinct from that of structurally related voltage-gated ion channels.
谷氨酸受体离子通道介导中枢神经系统大多数突触处的兴奋性反应。它们是唯一已解析出多个高分辨率晶体结构的配体门控离子通道。基于其配体结合域晶体结构的机制研究所得信息的亮点包括对显著多样现象的解释。这些现象包括亚型特异性激动剂选择性的基础；脱敏和变构调节机制；以及部分激动剂活性机制。此外，包括低分辨率电子显微镜研究在内的多条证据表明，天然AMPA受体与一个调节活性和转运的辅助亚基结合。功能研究表明，谷氨酸受体的门控与结构相关的电压门控离子通道不同。
