关键词: Block Ruthenium red TRP channels TRPV2 TRPV5 TRPV6

Mesh : Ruthenium Red / pharmacology metabolism TRPV Cation Channels / metabolism Transient Receptor Potential Channels

来  源:   DOI:10.1016/j.ceca.2024.102874

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.
摘要:
钌红(RR)是一种广泛使用的瞬时受体电位(TRP)阳离子通道和其他类型的离子通道抑制剂。虽然RR已被普遍接受通过物理阻断离子渗透途径来抑制TRP通道,最近的结构证据表明,它也可能起到拮抗剂的作用,在结合时诱导通道中的构象变化,从而导致孔的关闭。在最近发表在EMBO报告上的手稿中,RuthA.Pumroy和合作者在存在和不存在活化剂和RR的情况下解决了TRPV2和TRPV5通道的结构。这些数据揭示了RR抑制的机制,同时也为进一步调查开辟了新的问题。
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