Advances in Targeting GIRK Channels in Disease.
Advances in Targeting GIRK Channels in Disease.
复制标题
靶向疾病中GIRK通路的研究进展
DOI：
10.1016/j.tips.2020.12.002
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发表时间：
2021-03
影响因子：
13.8
通讯作者：
Slesinger PA
中科院分区：
文献类型：
--
作者：
Zhao Y;Gameiro-Ros I;Glaaser IW;Slesinger PA
G-protein-gated inwardly rectifying potassium (GIRK) channels are essential regulators of cell excitability in the brain. While implicated in a variety of neurological diseases in both human and animal model studies, their therapeutic potential has been largely untapped. Here, we review recent advances in the development of small molecule compounds that specifically modulate GIRK channels, and compare with first-generation compounds that exhibit off-target activity. We describe the method of discovery of these small molecule modulators, their chemical features, and their effects in vivo. These studies provide a promising outlook on future development of subunit-specific GIRK modulators to regulate neuronal excitability in a brain region-specific manner.
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影响因子：
25
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通讯作者：
Lüscher, C
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