期刊论文

The Structure and Molecular Pharmacology of Voltage-gated Calcium Channel Auxiliary Subunits α2δ-1

中文

中国生物化学与分子生物学报

1007-7626

2020

36

8

872-878

10.13865/j.cnki.cjbmb.2020.06.1074

湖南省教育厅基金会赠款(No.16A098) 湖南省科技厅重点科研项目(No.2017NK2311)资助。

本校为第一机构

电压门控钙通道(voltage-gated calcium channel,VGCC)辅助亚基α2δ-1在神经元兴奋传递中起促进作用,是加巴喷丁(gabapentin)和普瑞巴林(pregabalin)的作用靶点.α2δ-1由高度糖基化的α2亚基和δ亚基以4对二硫键相连,包含4个串联的Cache结构域和1个yon Willebrand A结构域,但δ亚基的C-末端结构尚未完全解析.α2δ-1的结构和作用机制研究进展主要聚焦于以下3点:(1) α2δ-1的C-末端,传统观点认为含有跨膜基序(motif).另一个观点认为是GPI锚定,尚缺乏直接的实验证明;(2)α2δ-1对电压门控钙离子通道的影响,包括直接的和非直接的调控对电压门控钙通道的膜上转运和电流的影响,以及α2δ-1的翻译后...

Voltage-gated calcium channel(VGCC) auxiliary subunits α2δ-1 plays a promoter in neuronal excitatory transmission and is the target of gabapentin and pregabalin. α2δ-1 is composed of highly glycosylated α2 and δ subunits connected by four pairs of disulfide bonds, including four Cache domains and a von Willebrand A domain, but the C-terminal structure of the δ subunit is not yet clear and controversial. The studies of the structure and mechanism of α2δ-1 mainly focus on the following three points:(1) The C-terminal of α2δ-1 is tradit...