Ruthenium red: Blocker or antagonist of TRPV channels?

IF 4.3 2区 生物学 Q2 CELL BIOLOGY Cell calcium Pub Date : 2024-03-18 DOI:10.1016/j.ceca.2024.102874
Andrés Jara-Oseguera
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Abstract

Ruthenium red (RR) is a widely used inhibitor of Transient Receptor Potential (TRP) cation channels and other types of ion channels. Although RR has been generally accepted to inhibit TRP channels by physically blocking the ion permeation pathway, recent structural evidence suggests that it might also function as an antagonist, inducing conformational changes in the channel upon binding that result in closure of the pore. In a recent manuscript published in EMBO Reports, Ruth A. Pumroy and collaborators solve structures of TRPV2 and TRPV5 channels in the presence and absence of activators and RR. The data sheds light on the mechanism of inhibition by RR, while also opening new questions for further investigation.

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钌红:TRPV 通道的阻断剂还是拮抗剂?
钌红(RR)是一种广泛使用的瞬态受体电位(TRP)阳离子通道和其他类型离子通道的抑制剂。虽然人们普遍认为钌红是通过物理方式阻断离子渗透途径来抑制 TRP 通道的,但最近的结构证据表明,它也可能发挥拮抗剂的作用,在与通道结合后诱导通道发生构象变化,从而导致孔道关闭。在最近发表于《EMBO Reports》的一篇手稿中,Ruth A. Pumroy 及其合作者解决了 TRPV2 和 TRPV5 通道在存在和不存在激活剂和 RR 的情况下的结构问题。这些数据揭示了 RR 的抑制机制,同时也提出了有待进一步研究的新问题。
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来源期刊
Cell calcium
Cell calcium 生物-细胞生物学
CiteScore
8.70
自引率
5.00%
发文量
115
审稿时长
35 days
期刊介绍: Cell Calcium covers the field of calcium metabolism and signalling in living systems, from aspects including inorganic chemistry, physiology, molecular biology and pathology. Topic themes include: Roles of calcium in regulating cellular events such as apoptosis, necrosis and organelle remodelling Influence of calcium regulation in affecting health and disease outcomes
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