配体门控离子通道受体别构调节研究  

Allosteric Modulation of Ligand-gated Ion Channel Receptor

作　　者：王颀[1] 周虎臣[1] 

机构地区：[1]上海交通大学药学院,上海200240

出　　处：《现代生物医学进展》2012年第30期5950-5953,5987,共5页Progress in Modern Biomedicine

基　　金：国家自然科学基金重大研究计划重点项目(2009CB918404;2009-2013)

摘　　要：配体门控离子通道(LGIC)在中枢神经系统信息处理的过程中起着极其重要的作用,与多种神经性疾病有着密切联系。与受体正位调节作用相比,别构调节效应具有类内源性生理作用、高选择性及不易过度调节的优点,从而避免了一系列不良反应发生。目前,各种LGIC受体超家族均有别构调节剂发现,部分已在临床上得到应用。在未来的研究中,通过建立及完善针对别构调节剂的筛选策略,别构调节剂的发现效率及生物活性将得到极大地提高,更多的药物将会不断涌现。Ligand-gated ion channels （LGIC） play an important role in the information processing of central nervous system （CNS）, and are closely bound up with several neurological diseases. Allosterie modulation boasts several advantages over orthosteric modulation due to the quiescence in the absence of endogenous activity, high selectivity and limited modulation effect. Nowadays, allosteric modulation effect is found in almost all the superfamilies of LGIC, and some allosteric modulators have been used clinically. In the following pharmaceutical research, the discovery efficiency and biological activity of allosteric modulators will be improved by developing good screening and design methods aiming at allostery.

关 键 词：别构调节 配体门控离子通道 神经性疾病 

分 类 号：Q593.2[生物学—生物化学] Q75