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解析血管平滑肌离子通道的复杂性:辅助亚基对活性的精细调节。

Unravelling the complexities of vascular smooth muscle ion channels: Fine tuning of activity by ancillary subunits.

机构信息

Department of Biomedical Sciences, University of Copenhagen, The Panum Institute, Blegdamsvej 3, 2200 Copenhagen N, Denmark.

出版信息

Pharmacol Ther. 2017 Oct;178:57-66. doi: 10.1016/j.pharmthera.2017.03.010. Epub 2017 Mar 21.

DOI:10.1016/j.pharmthera.2017.03.010
PMID:28336473
Abstract

Which ion channel is the most important for regulating vascular tone? Which one is responsible for controlling the resting membrane potential or repolarization? Which channels are recruited by different intracellular signalling pathways or change in certain vascular diseases? Many different ion channels have been identified in the vasculature over the years and claimed as future therapeutic targets. Unfortunately, several of these ion channels are not just found in the vasculature, with many of them also found to have prominent functional roles in different organs of the body, which then leads to off-target effects. As cardiovascular diseases are expected to increase worldwide to epidemic proportions, ion channel research and the hunt for the next major therapeutic target to treat different vascular diseases has never been more important. However, I believe that the question we should now be asking is: which ancillary subunits are involved in regulating specific ion channels in the vasculature and do they have the potential to be new therapeutic targets?

摘要

哪种离子通道对调节血管张力最重要?哪种离子通道负责控制静息膜电位或复极化?哪些通道被不同的细胞内信号通路募集或在某些血管疾病中发生变化?多年来,在血管中已经鉴定出许多不同的离子通道,并被认为是未来的治疗靶点。不幸的是,其中一些离子通道不仅存在于血管中,许多离子通道在体内的不同器官中也具有显著的功能作用,这就导致了脱靶效应。由于预计心血管疾病在全球范围内将增加到流行程度,因此离子通道研究和寻找下一个治疗不同血管疾病的主要治疗靶点从未如此重要。然而,我认为我们现在应该问的问题是:哪些辅助亚基参与调节血管中的特定离子通道,它们是否有可能成为新的治疗靶点?

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Unravelling the complexities of vascular smooth muscle ion channels: Fine tuning of activity by ancillary subunits.解析血管平滑肌离子通道的复杂性:辅助亚基对活性的精细调节。
Pharmacol Ther. 2017 Oct;178:57-66. doi: 10.1016/j.pharmthera.2017.03.010. Epub 2017 Mar 21.
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