Reducing GABA receptors.
Reducing GABA receptors.
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减少 GABA 受体。
DOI：
10.1016/s0024-3205(03)00505-8
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发表时间：
2003
期刊：
影响因子：
6.1
通讯作者：
Burt,DavidR
中科院分区：
文献类型：
--
作者：
Burt,DavidR
许多重要的药物作用于gaba受体，五聚体gaba门控氯通道由19个已知亚基组装而成。为了发现这些亚基及其组合在大脑中的作用，以开发更具选择性的药物为目标，一种工具是减少亚基的表达并检查其功能后果。在简要考察了gaba受体的性质之后，本文综述了受体亚基还原的可用手段，以及它们的应用所导致的一些观察结果。讨论的方法包括辐射诱导的缺失，基因敲除，敲入突变，反义，核酶，RNA干扰，显性负结构和转录调节，例如，通过诱饵寡核苷酸。
A number of important drugs act on GABAAreceptors, pentameric GABA-gated chloride channels assembled from among 19 known subunits. In trying to discover the roles in the brain of the subunits and their combinations, with the goal of developing more selective drugs, one tool has been to reduce expression of the subunits and examine the functional consequences. After briefly examining the properties of GABAAreceptors, this review surveys the means available for receptor subunit reduction, and some of the observations to which their application has led. The methods discussed include radiation-induced deletion, gene knockout, knock-in mutations, antisense, ribozymes, RNA interference, dominant negative constructs, and transcriptional regulation, e.g., via decoy oligonucleotides.