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硫化氢抑制Cav3.2 T型钙离子通道。

Hydrogen sulfide inhibits Cav3.2 T-type Ca2+ channels.

作者信息

Elies Jacobo, Scragg Jason L, Huang Sha, Dallas Mark L, Huang Dongyang, MacDougall David, Boyle John P, Gamper Nikita, Peers Chris

机构信息

Division of Cardiovascular and Diabetes Research, Leeds Institute of Cardiovascular and Metabolic Medicine, Faculty of Medicine and Health, and.

Department of Pharmacology, Hebei Medical University, Shijiazhuang, China; and.

出版信息

FASEB J. 2014 Dec;28(12):5376-87. doi: 10.1096/fj.14-257113. Epub 2014 Sep 2.

Abstract

The importance of H2S as a physiological signaling molecule continues to develop, and ion channels are emerging as a major family of target proteins through which H2S exerts many actions. The purpose of the present study was to investigate its effects on T-type Ca(2+) channels. Using patch-clamp electrophysiology, we demonstrate that the H2S donor, NaHS (10 μM-1 mM) selectively inhibits Cav3.2 T-type channels heterologously expressed in HEK293 cells, whereas Cav3.1 and Cav3.3 channels were unaffected. The sensitivity of Cav3.2 channels to H2S required the presence of the redox-sensitive extracellular residue H191, which is also required for tonic binding of Zn(2+) to this channel. Chelation of Zn(2+) with N,N,N',N'-tetra-2-picolylethylenediamine prevented channel inhibition by H2S and also reversed H2S inhibition when applied after H2S exposure, suggesting that H2S may act via increasing the affinity of the channel for extracellular Zn(2+) binding. Inhibition of native T-type channels in 3 cell lines correlated with expression of Cav3.2 and not Cav3.1 channels. Notably, H2S also inhibited native T-type (primarily Cav3.2) channels in sensory dorsal root ganglion neurons. Our data demonstrate a novel target for H2S regulation, the T-type Ca(2+) channel Cav3.2, and suggest that such modulation cannot account for the pronociceptive effects of this gasotransmitter.

摘要

硫化氢作为一种生理信号分子的重要性仍在不断深入研究,离子通道正逐渐成为硫化氢发挥多种作用的主要靶蛋白家族。本研究的目的是探究其对T型钙通道的影响。运用膜片钳电生理学技术,我们证明硫化氢供体硫氢化钠(10 μM - 1 mM)可选择性抑制在HEK293细胞中异源表达的Cav3.2 T型通道,而Cav3.1和Cav3.3通道不受影响。Cav3.2通道对硫化氢的敏感性需要氧化还原敏感的细胞外残基H191的存在,锌离子与该通道的张力结合也需要此残基。用N,N,N',N'-四-2-吡啶基乙二胺螯合锌离子可防止硫化氢对通道的抑制作用,并且在硫化氢暴露后再施加该螯合剂时,还可逆转硫化氢的抑制作用,这表明硫化氢可能通过增加通道对细胞外锌离子结合的亲和力来发挥作用。在3种细胞系中对天然T型通道的抑制作用与Cav3.2而非Cav3.1通道的表达相关。值得注意的是,硫化氢还抑制了感觉背根神经节神经元中的天然T型(主要是Cav3.2)通道。我们的数据证明了硫化氢调节的一个新靶点——T型钙通道Cav3.2,并表明这种调节不能解释这种气体递质的促痛觉效应。

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