摘要
作为半胱氨酸环配体门控离子通道中的一员,抑制性谷氨酸门控氯离子通道(IGluCl)的亚基及其装配具有多样性,从而导致其药理性质的不同。通道对某种化合物的选择性结合与通道中存在的一些关键位点的氨基酸残基有关。通道mRNA的转录后修饰作用是通道亚型及其功能多样化的原因。有关通道门控及离子选择机制的研究为新药及杀虫剂的开发和筛选奠定了基础。从药理性质、通道中影响药物结合特性的残基位点、通道基因的转录后修饰作用以及配体门控离子通道的门控机制等方面综述了IGluCl通道的研究情况。
Inhibitory glutamate-gated ion channels （IGluCls） are members of ＂Cys-loop＂ superfamily of ligand-gated ion channels. Diversity occurs in the subnnits and their assembly of IGluCls, which cause the variances in pharmacological properties. Certain key amino acids are linked to the selective ligand-binding of channels. Posttranscriptional mRNA modification can lead to extensive subtypes and functional diversification of channels. The study on mechanisms of channel gating and ion selectivity lay the foundation of new drugs and insecticides screening. The research progress of IGluC1 in pharmacological properties, residues implicated in drug binding, posttranscriptional mRNA modification and mechanisms of channel gating were reviewed.
出处
《世界农药》
CAS
2009年第3期4-10,共7页
World Pesticide
关键词
抑制性谷氨酸门控离子通道
药理性质
药物结合
转录后修饰
门控机制
inhibitory glutamate-gated ion channel （IGluRs）
pharmacological properties
drug binding
posttmnscriptional mRNA modification
mechanisms of channel gating
